List of works - 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

scientific article

A simple reaction to produce small structurally complex and diverse molecules

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

scientific article published on 02 June 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

scientific article published on 30 August 2013

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

scientific article

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

scientific article published on 30 May 2011

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

scientific article

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

scientific article published on 21 August 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

scientific article

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

scientific article published in April 1996

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

scientific article published on October 1997

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

scientific article published on 6 October 2017

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

scientific article

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

scientific article published on 2 August 2017

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

scientific article

Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds

scientific article published on 19 April 2011

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

scientific article

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

scientific article

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

scientific article published on April 2011

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

scientific article

Facts, figures and trends in lead generation

scientific article (publication date: 2004)

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

scientific article published on 02 March 2020

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

From hit to lead. Analyzing structure-profile relationships.

scientific article

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

scientific article

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

scientific article

Hydroxamates: relationships between structure and plasma stability

scientific article published in November 2009

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

scientific article

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

scientific article

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

scientific article published on April 2008

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

scientific article

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

scientific article

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

scientific article published on 20 April 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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article

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.

scientific article published on 28 February 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

scientific article published on 27 October 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.

scientific article

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

scientific article published on 31 August 2012

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

scientific article

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

scientific article published on 11 September 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

scientific article

Structural and docking studies of potent ethionamide boosters

scientific article published on 24 October 2013

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

scientific article published on 5 December 2012

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

scientific article

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

scientific article

The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity

scientific article published on 28 July 2015

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

scientific article published on 17 April 2017

Tuberculosis: the drug development pipeline at a glance

scientific article published on 25 February 2012

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

scientific article published on 20 February 2014

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

article published in 2013

List of works by 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