Lista de obras - Benoit Deprez - Dominio Público Uruguay

A facile and rapid synthesis of N-benzyl-2-substituted piperazines

A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening

artículo científico publicado en 2006

A simple reaction to produce small structurally complex and diverse molecules

ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease

artículo científico publicado en 2016

Access to newly functionalized imidazole derivatives: efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P)

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group

artículo científico publicado en 2013

Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds

artículo científico publicado en 2008

An ADAM protein as a new actor of the APP metabolism

Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation

artículo científico publicado en 2011

Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice

artículo científico publicado en 2015

Characterization of monoclonal antibodies by a fast and easy liquid chromatography-mass spectrometry time-of-flight analysis on culture supernatant

artículo científico publicado en 2015

ChemInform Abstract: Efficient Propylphosphonic Anhydride (®T3P) Mediated Synthesis of Benzothiazoles, Benzoxazoles and Benzimidazoles

ChemInform Abstract: Water-Based Conditions for the Microscale Parallel Synthesis of Bicyclic Lactams

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles

artículo científico publicado en 2017

Comparative efficiency of simple lipopeptide constructs for in vivo induction of virus-specific CTL.

artículo científico publicado en 1996

Confronting the degeneracy of convergent combinatorial immunogens, or 'mixotopes', with the specificity of recognition of the target sequences.

artículo científico publicado en 1997

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

artículo científico publicado en 2017

Designing focused chemical libraries enriched in protein-protein interaction inhibitors using machine-learning methods

artículo científico publicado en 2010

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

artículo científico publicado en 2017

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis

artículo científico publicado en 2012

Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds

artículo científico publicado en 2011

Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds

artículo científico publicado en 2012

Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis

scientific article published on 20 September 2018

Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles

Efficient, two-step synthesis of N-substituted nortropinone derivatives

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors

artículo científico publicado en 2012

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors

artículo científico publicado en 2011

Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator

artículo científico publicado en 2010

Facts, figures and trends in lead generation

artículo científico publicado en 2004

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity

artículo científico publicado en 2020

Friedländer synthesis of polysubstituted quinolines and naphthyridines promoted by propylphosphonic anhydride (T3P®) under mild conditions

From hit to lead. Analyzing structure-profile relationships.

artículo científico publicado en 2001

From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.

artículo científico publicado en 2001

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism

artículo científico publicado en 2016

Hydroxamates: relationships between structure and plasma stability

artículo científico publicado en 2009

Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737.

artículo científico publicado en 2014

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis

artículo científico publicado en 2014

In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics

artículo científico publicado en 2008

In vivo efficacy of microbiota-sensitive coatings for colon targeting: a promising tool for IBD therapy

artículo científico publicado en 2014

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

artículo científico publicado en 2014

Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion.

artículo científico publicado en 2015

Kinetic Target-Guided Synthesis: Reaching the Age of Maturity

scientific article published on 24 December 2019

Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey

artículo científico publicado en 2016

Lewis acid-induced reaction of homophthalic anhydride with imines: a convenient synthesis of trans-isoquinolonic acids

Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches

artículo científico publicado en 2014

Long-lasting anti-viral cytotoxic T lymphocytes induced in vivo with chimeric-multirestricted lipopeptides

scientific article published on 01 October 1995

MALDI imaging techniques dedicated to drug-distribution studies

artículo científico publicado en 2011

Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space

Natural compounds: leads or ideas? Bioinspired molecules for drug discovery

artículo científico publicado en 2008

New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold.

artículo científico publicado en 2010

Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives

artículo científico publicado en 2008

Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation

Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents.

artículo científico publicado en 2007

Orthogonal Combinatorial Chemical Libraries

article by Benoit Deprez et al published May 1995 in Journal of the American Chemical Society

PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil

artículo científico publicado en 2006

Pimelautide or trimexautide as built-in adjuvants associated with an HIV-1-derived peptide: synthesis and in vivo induction of antibody and virus-specific cytotoxic T-lymphocyte-mediated response.

artículo científico publicado en 1995

Preface [Hot topic: Hit-to-Lead: Driving Forces for the Medicinal Chemist (Guest Editor: Benoit Deprez and Rebecca Deprez-Poulain)]

Racemic and diastereoselective construction of indole alkaloids under solvent- and catalyst-free microwave-assisted Pictet–Spengler condensation

Rescue of nonsense mutations by amlexanox in human cells

artículo científico publicado en 2012

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.

artículo científico publicado en 2017

Setting Up a Bioluminescence Resonance Energy Transfer High throughput Screening Assay to Search for Protein/Protein Interaction Inhibitors in Mammalian Cells

artículo científico publicado en 2012

Solvent-free microwave-assisted Meyers’ lactamization

Squaric acid is a suitable building-block in 4C-Ugi reaction: access to original bivalent compounds

Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters

Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands

artículo científico publicado en 2012

Structural and docking studies of potent ethionamide boosters

artículo científico publicado en 2013

Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors

artículo científico publicado en 2012

Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.

artículo científico publicado en 2014

Synthesis and structural studies of a novel scaffold for drug discovery: a 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine]

Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann–Finkelstein tandem reaction

Synthesis of five- and six-membered lactams via solvent-free microwave Ugi reaction

Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

artículo científico publicado en 2009

The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity

artículo científico publicado en 2015

Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance

artículo científico publicado en 2017

Tuberculosis: the drug development pipeline at a glance

artículo científico

UFU (‘Ullmann–Finkelstein–Ullmann’): a new multicomponent reaction

Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil

Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands

artículo científico publicado en 2014

Water-based conditions for the microscale parallel synthesis of bicyclic lactams

article published in 2013

Lista de obras de Benoit Deprez

A facile and rapid synthesis of N-benzyl-2-substituted piperazines

A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening

A simple reaction to produce small structurally complex and diverse molecules

ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease

Access to newly functionalized imidazole derivatives: efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P)

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group

Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds

An ADAM protein as a new actor of the APP metabolism

Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation

Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice

Characterization of monoclonal antibodies by a fast and easy liquid chromatography-mass spectrometry time-of-flight analysis on culture supernatant

ChemInform Abstract: Efficient Propylphosphonic Anhydride (®T3P) Mediated Synthesis of Benzothiazoles, Benzoxazoles and Benzimidazoles

ChemInform Abstract: Water-Based Conditions for the Microscale Parallel Synthesis of Bicyclic Lactams

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles

Comparative efficiency of simple lipopeptide constructs for in vivo induction of virus-specific CTL.

Confronting the degeneracy of convergent combinatorial immunogens, or 'mixotopes', with the specificity of recognition of the target sequences.

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

Designing focused chemical libraries enriched in protein-protein interaction inhibitors using machine-learning methods

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis

Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds

Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds

Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis

Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles

Efficient, two-step synthesis of N-substituted nortropinone derivatives

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors

Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator

Facts, figures and trends in lead generation

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity

Friedländer synthesis of polysubstituted quinolines and naphthyridines promoted by propylphosphonic anhydride (T3P®) under mild conditions

From hit to lead. Analyzing structure-profile relationships.

From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands.

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism

Hydroxamates: relationships between structure and plasma stability

Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737.

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis

In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics

In vivo efficacy of microbiota-sensitive coatings for colon targeting: a promising tool for IBD therapy

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion.

Kinetic Target-Guided Synthesis: Reaching the Age of Maturity

Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey

Lewis acid-induced reaction of homophthalic anhydride with imines: a convenient synthesis of trans-isoquinolonic acids

Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches

Long-lasting anti-viral cytotoxic T lymphocytes induced in vivo with chimeric-multirestricted lipopeptides

MALDI imaging techniques dedicated to drug-distribution studies

Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space

Natural compounds: leads or ideas? Bioinspired molecules for drug discovery

New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold.

Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives

Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation

Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents.

Orthogonal Combinatorial Chemical Libraries

PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil

Pimelautide or trimexautide as built-in adjuvants associated with an HIV-1-derived peptide: synthesis and in vivo induction of antibody and virus-specific cytotoxic T-lymphocyte-mediated response.

Preface [Hot topic: Hit-to-Lead: Driving Forces for the Medicinal Chemist (Guest Editor: Benoit Deprez and Rebecca Deprez-Poulain)]

Racemic and diastereoselective construction of indole alkaloids under solvent- and catalyst-free microwave-assisted Pictet–Spengler condensation

Rescue of nonsense mutations by amlexanox in human cells

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.

Setting Up a Bioluminescence Resonance Energy Transfer High throughput Screening Assay to Search for Protein/Protein Interaction Inhibitors in Mammalian Cells

Solvent-free microwave-assisted Meyers’ lactamization

Squaric acid is a suitable building-block in 4C-Ugi reaction: access to original bivalent compounds

Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters

Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands

Structural and docking studies of potent ethionamide boosters

Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors

Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.

Synthesis and structural studies of a novel scaffold for drug discovery: a 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine]

Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann–Finkelstein tandem reaction

Synthesis of five- and six-membered lactams via solvent-free microwave Ugi reaction

Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity

Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance

Tuberculosis: the drug development pipeline at a glance

UFU (‘Ullmann–Finkelstein–Ullmann’): a new multicomponent reaction

Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil

Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands