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4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species

artículo científico publicado en 2006

A liquid chromatography high-resolution mass spectrometry in vitro assay to assess metabolism at the injection site of subcutaneously administered therapeutic peptides

artículo científico publicado en 2018

A novel method using nuclear magnetic resonance for plasma protein binding assessment in drug discovery programs

scientific article published on 31 January 2019

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo

artículo científico publicado en 2008

A novel strategy for reducing phospholipids-based matrix effect in LC-ESI-MS bioanalysis by means of HybridSPE.

artículo científico publicado en 2009

A single-run liquid chromatography mass spectrometry method to quantify neuroactive kynurenine pathway metabolites in rat plasma

artículo científico publicado en 2015

An efficient liquid chromatography-high resolution mass spectrometry approach for the optimization of the metabolic stability of therapeutic peptides.

artículo científico publicado en 2017

ApoA-I mimetic peptides promote pre-β HDL formation in vivo causing remodeling of HDL and triglyceride accumulation at higher dose

artículo científico publicado en 2010

Application of an in Vitro Blood-Brain Barrier Model in the Selection of Experimental Drug Candidates for the Treatment of Huntington's Disease

scientific article published on 04 April 2019

Conformations of laulimalide in DMSO-d6.

artículo científico publicado en 2005

DPP‐IV‐resistant, long‐acting oxyntomodulin derivatives

artículo científico publicado el 3 de febrero de 2011

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors

artículo científico publicado en 2008

Determination of acetyl coenzyme A in human whole blood by ultra-performance liquid chromatography-mass spectrometry.

artículo científico publicado en 2018

Development of a neuromedin U-human serum albumin conjugate as a long-acting candidate for the treatment of obesity and diabetes. Comparison with the PEGylated peptide

artículo científico publicado en 2013

Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells

scientific article published on 22 November 2009

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors

artículo científico publicado en 2007

Discovery and Characterization of Novel Anti-schistosomal Properties of the Anti-anginal Drug, Perhexiline and Its Impact on Schistosoma mansoni Male and Female Reproductive Systems

artículo científico publicado en 2016

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones

artículo científico publicado en 2007

Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors

artículo científico publicado en 2009

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor

artículo científico publicado en 2012

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs

artículo científico publicado en 2016

Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties

artículo científico publicado en 2009

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection

artículo científico publicado en 2008

Enhanced mass resolution method development, validation and assay application to support preclinical studies of a new drug candidate

artículo científico publicado en 2006

Enhancement of intestinal absorption of 2-methyl cytidine prodrugs

artículo científico publicado en 2010

Establishment of an in Vitro Human Blood-Brain Barrier Model Derived from Induced Pluripotent Stem Cells and Comparison to a Porcine Cell-Based System

scientific article published on 16 April 2020

Fosmetpantotenate (RE-024), a phosphopantothenate replacement therapy for pantothenate kinase-associated neurodegeneration: Mechanism of action and efficacy in nonclinical models.

artículo científico publicado en 2018

HILIC LC-MS for the determination of 2'-C-methyl-cytidine-triphosphate in rat liver

artículo científico publicado en 2009

High sensitivity determination of valproic acid in mouse plasma using semi-automated sample preparation and liquid chromatography with tandem mass spectrometric detection

artículo científico publicado en 2005

High-throughput microsomal stability assay for screening new chemical entities in drug discovery

artículo científico publicado en 2008

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies

artículo científico publicado el 16 de junio de 2011

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides

scientific article published on 27 November 2018

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants.

artículo científico publicado en 2014

MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants

artículo científico publicado en 2012

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists

artículo científico publicado en 2011

Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement

artículo científico publicado en 2009

PEGylation of Neuromedin U yields a promising candidate for the treatment of obesity and diabetes

artículo científico publicado en 2012

Quantitative prediction of human clearance guiding the development of Raltegravir (MK-0518, isentress) and related HIV integrase inhibitors

artículo científico publicado en 2009

Synthesis and Biological Evaluation of RGD⁻Cryptophycin Conjugates for Targeted Drug Delivery

artículo científico publicado en 2019

Synthesis and antiviral properties of novel 7-heterocyclic substituted 7-deaza-adenine nucleoside inhibitors of Hepatitis C NS5B polymerase

artículo científico publicado el 6 de junio de 2012

Synthesis, biological evaluation, and molecular modeling studies of rebeccamycin analogues modified in the carbohydrate moiety

artículo científico

The synthesis of tetrahydropyridopyrimidones as a new scaffold for HIV-1 integrase inhibitors

article

Turbulent flow chromatography TFC-tandem mass spectrometry supporting in vitro/vivo studies of NCEs in high throughput fashion

artículo científico publicado en 2009

Use of 'dilute-and-shoot' liquid chromatography-high resolution mass spectrometry in preclinical research: application to a DMPK study of perhexiline in mouse plasma.

artículo científico publicado en 2015