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Lista de obras de Alan P. Kozikowski

1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties

artículo científico publicado en 1999

11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase).

artículo científico publicado en 2002

18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboons

artículo científico publicado en 2009

2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors

artículo científico publicado en 2003

2,3-disubstituted 6-azabicyclo[3.2.1]octanes as novel dopamine transporter inhibitors

artículo científico publicado en 2004

2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics

scientific article published on 24 October 2018

3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth

artículo científico publicado en 2000

5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice.

artículo científico publicado en 2017

A Novel Role for Histone Deacetylase 6 (HDAC6) in the Regulation of IL-10 and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs). ⬇️

scholarly article

A Short and Efficient Synthesis of the Pharmacological Research Tool GW501516 for the Peroxisome Proliferator-Activated Receptor δ ⬇️

artículo científico publicado el 14 de noviembre de 2003

A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents

artículo científico publicado en 2000

A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas

artículo científico publicado en 2013

A novel role for histone deacetylase 6 in the regulation of the tolerogenic STAT3/IL-10 pathway in APCs.

artículo científico publicado en 2014

A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019)

scientific article published on 25 December 2019

A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer

artículo científico publicado en 2009

A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum

artículo científico publicado en 2008

A versatile approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from L-(-)-quebrachitol

artículo científico publicado en 2000

ATPS-91GSK-3 INHIBITOR 9-ING-41 ENHANCES GENOTOXIC THERAPY OF GBM LEADING TO CURE FROM INTRACRANIAL BRAIN TUMOR.

artículo científico publicado en 2015

Abstract LB-074: Priming the tumor microenvironment with epigenetic modifiers to overcome resistance to immune checkpoint inhibitors

scholarly article

Acetylenic pyridines for use in PET imaging of nicotinic receptors.

artículo científico publicado en 2007

Active Benzimidazole Derivatives Targeting the MmpL3 Transporter in Mycobacterium abscessus

artículo científico publicado en 2020

Advancing the Therapeutic Potential of Indoleamides for Tuberculosis

scientific article published on 24 June 2019

An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes

artículo científico publicado en 2000

An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity.

artículo científico publicado en 2012

Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors

artículo científico publicado en 2008

Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model

artículo científico publicado en 2004

Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor

artículo científico publicado en 2007

Author Correction: Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells

scientific article published on 10 October 2019

Biaryl Analogues of Conformationally Constrained Tricyclic Tropanes as Potent and Selective Norepinephrine Reuptake Inhibitors: Synthesis and Evaluation of Their Uptake Inhibition at Monoamine Transporter Sites ⬇️

artículo científico publicado el 8 de mayo de 2003

Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot-Marie-Tooth Disease

artículo científico publicado en 2015

Biodistribution, tumor detection, and radiation dosimetry of 18F-DCFBC, a low-molecular-weight inhibitor of prostate-specific membrane antigen, in patients with metastatic prostate cancer

artículo científico publicado en 2012

Biological evaluation of potent triclosan-derived inhibitors of the enoyl-acyl carrier protein reductase InhA in drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis

artículo científico publicado en 2014

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome

artículo científico publicado en 2018

Cellular pharmacology of D-3-azido-3-deoxy-myo-inositol, an inhibitor of phosphatidylinositol signaling having antiproliferative activity

artículo científico publicado en 1994

Characterization of Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitors as Stimulators of Steroidogenesis ⬇️

artículo científico publicado el 17 de junio de 2013

Chemical medicine: novel 10-substituted cytisine derivatives with increased selectivity for alpha4beta2 nicotinic acetylcholine receptors

scientific article published on 01 August 2007

Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects

artículo científico publicado en 2000

Chemistry and Behavioral Studies Identify Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile ⬇️

artículo científico publicado el 10 de enero de 2012

Chemistry and Biology of the 2.beta.-Alkyl-3.beta.-phenyl Analogs of Cocaine: Subnanomolar Affinity Ligands That Suggest a New Pharmacophore Model at the C-2 Position ⬇️

artículo científico publicado el 4 de agosto de 1995

Chemistry and Pharmacology of the Piperidine-Based Analogues of Cocaine. Identification of Potent DAT Inhibitors Lacking the Tropane Skeleton ⬇️

artículo científico publicado el 21 de mayo de 1998

Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors

scientific article published on 01 March 2005

Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as α4β2-nicotinic acetylcholine receptor-selective partial agonists.

artículo científico publicado en 2010

Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression

artículo científico publicado en 2009

Chemistry, Pharmacology, and Behavioral Studies Identify Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part II ⬇️

artículo científico publicado el 26 de junio de 2013

Chemistry, biology, and QSAR studies of substituted biaryl hydroxamates and mercaptoacetamides as HDAC inhibitors-nanomolar-potency inhibitors of pancreatic cancer cell growth

artículo científico publicado en 2008

Chiral Mercaptoacetamides Display Enantioselective Inhibition of Histone Deacetylase 6 and Exhibit Neuroprotection in Cortical Neuron Models of Oxidative Stress

scientific article published on 10 January 2012

CoMFA study of piperidine analogues of cocaine at the dopamine transporter: exploring the binding mode of the 3 alpha-substituent of the piperidine ring using pharmacophore-based flexible alignment

artículo científico publicado en 2004

Cocaine and dopamine differentially protect [3H]mazindol binding sites from alkylation by N-ethylmaleimide

artículo científico publicado el 1 de diciembre de 1992

Combination Treatment with the GSK-3 Inhibitor 9-ING-41 and CCNU Cures Orthotopic Chemoresistant Glioblastoma in Patient-Derived Xenograft Models

artículo científico publicado en 2017

Complete (1)H NMR spectral fingerprint of huperzine A.

artículo científico publicado en 2007

Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors

artículo científico publicado en 2019

Controlling Extra- and Intramacrophagic Mycobacterium abscessus by Targeting Mycolic Acid Transport

artículo científico publicado en 2017

Defining the minimal structural requirements for partial agonism at the type I myo-inositol 1,4,5-trisphosphate receptor

scientific article published on 01 February 1997

Derivatives of 3-isoxazolecarboxylic acid esters: a potent and selective compound class against replicating and nonreplicating Mycobacterium tuberculosis

artículo científico

Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists

artículo científico publicado en 2016

Design and Synthesis of (2-(5-Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist

artículo científico publicado en 2015

Design and Synthesis of Aryl Ether Inhibitors of theBacillus AnthracisEnoyl-ACP Reductase

artículo científico publicado en 2008

Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands

artículo científico publicado en 2020

Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors

artículo científico publicado en 2017

Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.

artículo científico publicado en 2008

Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy

artículo científico publicado en 2006

Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.

artículo científico publicado en 2004

Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population

artículo científico publicado en 2004

Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism

artículo científico publicado en 2019

Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase)

artículo científico publicado en 2001

Design, Synthesis, and Pharmacological Evaluation of Mefloquine-Based Ligands as Novel Antituberculosis Agents

scientific article published on 01 November 2007

Design, Synthesis, and SAR Studies of Mefloquine-Based Ligands as Potential Antituberculosis Agents

scientific article published on 01 June 2006

Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51.

artículo científico publicado en 2016

Development of new brain imaging agents based upon nocaine-modafinil hybrid monoamine transporter inhibitors

artículo científico publicado en 2006

Differential binding and dopamine uptake activity of cocaine analogues modified at nitrogen

artículo científico publicado en 1994

Dipolar Cycloaddition Route to Diverse Analogues of Cocaine: The 6- and 7-Substituted 3-Phenyltropanes ⬇️

artículo científico publicado el 7 de febrero de 1997

Discovery of Highly Potent and Selective α4β2-Nicotinic Acetylcholine Receptor (nAChR) Partial Agonists Containing an Isoxazolylpyridine Ether Scaffold that Demonstrate Antidepressant-like Activity. Part II ⬇️

artículo científico publicado el 2 de noviembre de 2012

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.

artículo científico publicado en 2017

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models

artículo científico publicado en 2019

Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression

artículo científico publicado en 2011

Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants

artículo científico publicado en 2005

Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay

artículo científico publicado en 2013

Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380.

artículo científico publicado en 2011

Divergent roles of histone deacetylase 6 (HDAC6) and histone deacetylase 11 (HDAC11) on the transcriptional regulation of IL10 in antigen presenting cells

artículo científico publicado en 2014

Dopaminergic agents for the treatment of cocaine abuse

artículo científico publicado en 1999

Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity

artículo científico publicado en 2000

Dysregulation of glutamate carboxypeptidase II in psychiatric disease.

artículo científico publicado en 2008

Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands

artículo científico publicado en 2014

Epigenetic regulation of autophagy by the methyltransferase G9a

scientific journal article

Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer ⬇️

artículo científico

Exploration of the labeling of [11C]tubastatin A at the hydroxamic acid site with [11C]carbon monoxide.

artículo científico publicado en 2015

From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells

artículo científico publicado en 2009

From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters

artículo científico publicado en 2009

From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.

artículo científico publicado en 2012

Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies

artículo científico publicado en 2007

Functionalization of the alicyclic skeleton of epibatidine: synthesis and nicotinic acetylcholine receptor binding affinities of epibatidine analogues

artículo científico publicado en 2003

Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.

artículo científico publicado en 2015

Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors

artículo científico publicado en 2000

Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin t

artículo científico publicado en 2002

GSK-3 inhibition overcomes chemoresistance in human breast cancer

artículo científico publicado en 2016

GSK-3β Governs Inflammation-Induced NFATc2 Signaling Hubs to Promote Pancreatic Cancer Progression

artículo científico publicado en 2016

Glutamate carboxypeptidase II levels in rodent brain using [125I]DCIT quantitative autoradiography

artículo científico publicado en 2005

Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP1/ATR-Mediated DNA Damage Response

scientific article published on 18 September 2019

HDAC6 inhibition promotes α-tubulin acetylation and ameliorates CMT2A peripheral neuropathy in mice

scientific article published on 05 March 2020

HDAC6 inhibitors reverse axonal loss in a mouse model of mutant HSPB1–induced Charcot-Marie-Tooth disease

article

HDAC6 is a target for protection and regeneration following injury in the nervous system

artículo científico publicado en 2009

HDAC6 is a therapeutic target in mutant GARS-induced Charcot-Marie-Tooth disease.

artículo científico publicado en 2018

HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia

artículo científico publicado en 2010

HTS, chemical hybridization, and drug design identify a chemically unique antituberculosis agent-coupling serendipity and rational approaches to drug discovery

artículo científico publicado en 2007

Highly potent and specific GSK-3beta inhibitors that block tau phosphorylation and decrease alpha-synuclein protein expression in a cellular model of Parkinson's disease.

artículo científico publicado en 2006

Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells

artículo científico publicado en 2011

Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition.

artículo científico publicado en 2014

Histone/protein deacetylase 11 targeting promotes Foxp3+ Treg function.

artículo científico publicado en 2017

Identification and Development of Novel Inhibitors of Toxoplasma gondii Enoyl Reductase

artículo científico publicado en 2010

Identification of HDAC6-Selective Inhibitors of Low Cancer Cell Cytotoxicity

artículo científico publicado en 2015

Identification of Novel α4β2-Nicotinic Acetylcholine Receptor (nAChR) Agonists Based on an Isoxazole Ether Scaffold that Demonstrate Antidepressant-like Activity ⬇️

artículo científico publicado el 4 de enero de 2012

Identification of a Glycogen Synthase Kinase‐3β Inhibitor that Attenuates Hyperactivity in CLOCK Mutant Mice ⬇️

artículo científico publicado el 5 de julio de 2011

Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy.

artículo científico publicado en 2012

Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents

artículo científico publicado en 2010

In pursuit of natural product leads: synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and its analogues: discovery of N-(2-benzoxazol-2-ylphenyl)benzamides as n

artículo científico publicado en 2008

Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection

artículo científico publicado en 2016

Indoleamides are active against drug-resistant Mycobacterium tuberculosis

artículo científico publicado en 2013

Inhibition of GSK-3 induces differentiation and impaired glucose metabolism in renal cancer.

artículo científico publicado en 2013

Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands

artículo científico publicado en 2012

Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization

artículo científico publicado en 2008

Intracerebroventricular administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in inflammatory pain

artículo científico publicado en 2008

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity

artículo científico publicado en 2009

Isoxazolyl-serine-based agonists of peroxisome proliferator-activated receptor: design, synthesis, and effects on cardiomyocyte differentiation

artículo científico publicado en 2004

Ketamine and N-acetylaspartylglutamate peptidase inhibitor exert analgesia in bone cancer pain

artículo científico publicado en 2006

Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats

artículo científico publicado en 2007

Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors

scientific article published on 29 September 2020

Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist".

artículo científico publicado en 1993

Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine

artículo científico publicado en 2003

Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme sele

artículo científico publicado en 1997

Modification of the side chain of micromolide, an anti-tuberculosis natural product

artículo científico publicado en 2008

Modification of triclosan scaffold in search of improved inhibitors for enoyl-acyl carrier protein (ACP) reductase in Toxoplasma gondii

artículo científico publicado en 2013

Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor

scientific article published on 21 November 2018

Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer

artículo científico publicado en 2017

Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors

artículo científico publicado en 2002

Molecular modeling, structure--activity relationships and functional antagonism studies of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketones as a novel class of dopamine transporter inhibitors.

artículo científico publicado en 2001

Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors

artículo científico publicado en 2008

Mutation of Rv2887, a marR-like gene, confers Mycobacterium tuberculosis resistance to an imidazopyridine-based agent.

artículo científico publicado en 2015

N-[N-[(S)-1,3-Dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine, [18F]DCFBC: a new imaging probe for prostate cancer

artículo científico publicado en 2008

N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter

artículo científico publicado en 1999

NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR.

artículo científico publicado en 2004

NAAG peptidase inhibitor increases dialysate NAAG and reduces glutamate, aspartate and GABA levels in the dorsal hippocampus following fluid percussion injury in the rat.

artículo científico publicado en 2006

NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats

artículo científico publicado en 2005

NAAG peptidase inhibitors and their potential for diagnosis and therapy

artículo científico publicado en 2005

NOC chemistry for tuberculosis-further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

artículo científico publicado en 2010

Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents ⬇️

artículo científico publicado en 2009

Neuroprotective and nootropic actions of a novel cyclized dipeptide after controlled cortical impact injury in mice

artículo científico publicado en 2003

New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha

artículo científico publicado en 2003

New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity

artículo científico publicado en 2003

Novel HDAC inhibitors with radiosensitizing properties

artículo científico publicado en 2005

Novel N-benzoyl-2-hydroxybenzamide disrupts unique parasite secretory pathway

artículo científico publicado en 2012

Novel PI analogues selectively block activation of the pro-survival serine/threonine kinase Akt.

artículo científico publicado en 2003

Novel Peptidomimetic Cysteine Protease Inhibitors as Potential Antimalarial Agents

artículo científico publicado en 2006

Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter

artículo científico publicado en 2000

Novel diketopiperazine enhances motor and cognitive recovery after traumatic brain injury in rats and shows neuroprotection in vitro and in vivo

artículo científico publicado en 2003

Novel inhibitors of human histone deacetylase (HDAC) identified by QSAR modeling of known inhibitors, virtual screening, and experimental validation

artículo científico publicado en 2009

Novel monoamine transporter ligands reduce cocaine-induced enhancement of brain stimulation reward

artículo científico publicado en 2001

Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits

artículo científico publicado en 2005

Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents

artículo científico publicado en 2015

Optimization of Drug Candidates That Inhibit the D-Loop Activity of RAD51

artículo científico publicado en 2019

Palladium catalyzed synthesis of annelated indoles ⬇️

scholarly article

Peroxisome proliferator-activated receptor delta and gamma agonists differentially alter tumor differentiation and progression during mammary carcinogenesis

artículo científico publicado en 2005

Pharmacokinetics and brain penetration of LF-3-88, (2-[5-[5-(2(S)-azetidinylmethoxyl)-3-pyridyl]-3-isoxazolyl]ethanol), a selective α4β2-nAChR partial agonist and promising antidepressant

artículo científico publicado en 2012

Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors

artículo científico publicado en 2001

Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.

artículo científico publicado en 2001

Phencyclidine and dizocilpine induced behaviors reduced by N-acetylaspartylglutamate peptidase inhibition via metabotropic glutamate receptors

artículo científico publicado en 2007

Phosphatidylinositol ether lipid analogues induce AMP-activated protein kinase-dependent death in LKB1-mutant non small cell lung cancer cells

artículo científico publicado en 2008

Phosphatidylinositol ether lipid analogues that inhibit AKT also independently activate the stress kinase, p38alpha, through MKK3/6-independent and -dependent mechanisms.

artículo científico publicado en 2007

Physical Interaction of Histone Deacetylase 6 (HDAC6) with STAT3 Regulates IL-10 Gene Expression and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs) ⬇️

scholarly article

Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.

artículo científico publicado en 2004

Preferential inhibition of Akt and killing of Akt-dependent cancer cells by rationally designed phosphatidylinositol ether lipid analogues

artículo científico publicado en 2004

Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains

artículo científico publicado en 2013

Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations

artículo científico publicado en 1999

Putting the 'HAT' back on survival signalling: the promises and challenges of HDAC inhibition in the treatment of neurological conditions

scientific article published on 01 May 2009

Pyrido[1,2-a]benzimidazole-based agents active against tuberculosis (TB), multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB

artículo científico publicado en 2011

RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells

artículo científico publicado en 2012

Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer

artículo científico publicado en 2005

Rational Design of Suprastat, a Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

artículo científico publicado en 2020

Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity

artículo científico publicado en 2011

Rational design and development of radiation-sensitizing histone deacetylase inhibitors

artículo científico publicado en 2005

Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A

artículo científico publicado en 2010

Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development

artículo científico publicado en 2010

Recent Developments Using Small Molecules to Target RAD51: How to Best Modulate RAD51 for Anticancer Therapy?

artículo científico publicado en 2016

Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors

artículo científico publicado en 2014

Role of the increased noradrenergic neurotransmission in drug self-administration

artículo científico publicado en 2006

SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement

artículo científico publicado en 2002

Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles

artículo científico publicado en 2001

Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them

artículo científico publicado en 2006

Searching for disease modifiers-PKC activation and HDAC inhibition - a dual drug approach to Alzheimer's disease that decreases Abeta production while blocking oxidative stress

artículo científico publicado en 2009

Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles

artículo científico publicado en 2009

Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells

artículo científico publicado en 2012

Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action

artículo científico publicado en 2009

Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells

artículo científico publicado en 2019

Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.

artículo científico publicado en 2012

Spectrum of activity and molecular correlates of response to phosphatidylinositol ether lipid analogues, novel lipid-based inhibitors of Akt.

artículo científico publicado en 2006

Stereochemistry at the forefront in the design and discovery of novel anti-tuberculosis agents

artículo científico publicado en 2011

Stereoselective HDAC inhibition from cysteine-derived zinc-binding groups.

artículo científico publicado en 2009

Structural analogs of huperzine A improve survival in guinea pigs exposed to soman

artículo científico publicado en 2012

Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor

scientific article published on 15 January 2020

Structural basis of RasGRP binding to high-affinity PKC ligands.

artículo científico publicado en 2002

Structural remodeling of cocaine: design and synthesis of trisubstituted cyclopropanes as selective serotonin reuptake inhibitors

artículo científico publicado en 2006

Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding

artículo científico publicado en 1994

Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue

artículo científico publicado el 11 de diciembre de 1992

Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.

artículo científico publicado en 2009

Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase

artículo científico publicado en 2008

Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. possible new GSK-3beta therapies for bipolar disorders

artículo científico publicado en 2007

Structure-guided design of a highly selective glycogen synthase kinase-3β inhibitor: a superior neuroprotective pyrazolone showing antimania effects

artículo científico publicado en 2011

Studies in polyphenol chemistry and bioactivity. 4.(1) Synthesis of trimeric, tetrameric, pentameric, and higher oligomeric epicatechin-derived procyanidins having all-4beta,8-interflavan connectivity and their inhibition of cancer cell growth throu

artículo científico publicado en 2003

Studies of benzamide- and thiol-based histone deacetylase inhibitors in models of oxidative-stress-induced neuronal death: identification of some HDAC3-selective inhibitors

artículo científico publicado en 2009

Synergistic interactions of indole-2-carboxamides and β-lactam antibiotics against Mycobacterium abscessus

artículo científico publicado en 2020

Synthesis and Akt inhibitory properties of a 1d-3,4-dideoxyphosphatidylinositol ether lipid ⬇️

scholarly article

Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III.

artículo científico publicado en 2016

Synthesis and Biology of the Conformationally Restricted ACPD Analogue, 2-Aminobicyclo[2.1.1]hexane-2,5-dicarboxylic Acid-I, a Potent mGluR Agonist ⬇️

artículo científico publicado el 7 de mayo de 1998

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models

artículo científico publicado en 2017

Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring

scientific article published on 01 June 1998

Synthesis and biological activity of novel neuroprotective diketopiperazines

artículo científico publicado en 2002

Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors

artículo científico publicado en 2000

Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.

artículo científico publicado en 2016

Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents

artículo científico publicado en 2010

Synthesis and biological evaluation of two analogues of (S)-alpha-methyl-3-carboxyphenylalanine

artículo científico publicado en 1998

Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine

artículo científico publicado en 1999

Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters

artículo científico publicado en 1998

Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation

scientific article published on 01 March 1995

Synthesis and biology of a 7-nitro-2,1,3-benzoxadiazol-4-yl derivative of 2-phenylindole-3-acetamide: a fluorescent probe for the peripheral-type benzodiazepine receptor

artículo científico publicado en 1997

Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter

artículo científico publicado en 2003

Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA).

artículo científico publicado en 2008

Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation

artículo científico publicado en 1998

Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives

scientific article published on 01 September 1993

Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators

artículo científico publicado en 2002

Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors

artículo científico publicado en 2004

Synthesis and pharmacological evaluation of ( Z )-9-(Heteroarylmethylene)-7-azatricyclo[4.3.1.0 3,7 ]decanes: thiophene analogues as potent norepinephrine transporter inhibitors ⬇️

artículo científico publicado el 20 de octubre de 2003

Synthesis and pharmacological evaluation of 8- and 9-substituted benzolactam-v8 derivatives as potent ligands for protein kinase C, a therapeutic target for Alzheimer's disease

artículo científico publicado en 2006

Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity

artículo científico publicado en 2006

Synthesis and protein kinase C binding activity of benzolactam-V7

scientific article published on 01 May 1999

Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications

artículo científico publicado en 2006

Synthesis of 7-substituted benzolactam-V8s and their selectivity for protein kinase C isozymes

scientific article published on 01 July 2002

Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.

artículo científico publicado en 1999

Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B

scientific article published on 01 June 2002

Synthesis of novel spirocyclic cocaine analogs using the Suzuki coupling

Synthesis of the benzofuran analogue of ILV, a new protein kinase C (PKC) activator

scholarly article

Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents

artículo científico publicado en 2004

Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.

artículo científico publicado en 2009

Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania

artículo científico publicado en 2012

Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A

scientific article published on 01 November 2000

Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring

artículo científico publicado en 2004

Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues

artículo científico publicado en 2003

Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.

artículo científico publicado en 2017

The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors

artículo científico publicado en 2014

The amino terminus of tau inhibits kinesin-dependent axonal transport: implications for filament toxicity.

artículo científico publicado en 2009

The novel triple reuptake inhibitor JZAD-IV-22 exhibits an antidepressant pharmacological profile without locomotor stimulant or sensitization properties

artículo científico publicado en 2010

The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.

artículo científico publicado en 2014

The preclinical candidate indole-2-carboxamide improves immune responses to Mycobacterium tuberculosis infection in healthy subjects and individuals with type 2 diabetes

scholarly article by Ruoqiong Cao et al published 19 June 2019 in International Microbiology

Thiol-Based Potent and Selective HDAC6 Inhibitors Promote Tubulin Acetylation and T-Regulatory Cell Suppressive Function

artículo científico publicado en 2015

Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors

artículo científico publicado en 2002

Tubastatin A, an HDAC6 inhibitor, alleviates stroke-induced brain infarction and functional deficits: potential roles of α-tubulin acetylation and FGF-21 up-regulation

artículo científico publicado en 2016

Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors

artículo científico publicado en 2009

Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.

artículo científico publicado en 2008

Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation

artículo científico publicado en 2010

We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.

artículo científico publicado en 2015

Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors--What Some May Have Forgotten or Would Rather Forget?

artículo científico publicado en 2015

Why academic drug discovery makes sense

artículo científico publicado en 2006

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