List of works - Rébecca F Déprez-Poulain

1,4-bis(3-aminopropyl)piperazine libraries: from the discovery of classical chloroquine-like antimalarials to the identification of new targets.

scientific article published in February 2005

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

A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues

ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion

scientific article published on 7 July 2016

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

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

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

scientific article published on 6 October 2017

Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.

scientific article published on 21 February 2017

Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.

scientific article

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

Ensemble cryoEM elucidates the mechanism of insulin capture and degradation by human insulin degrading enzyme

scientific article published on 29 March 2018

Facts, figures and trends in lead generation

scientific article (publication date: 2004)

Hydroxamates: relationships between structure and plasma stability

scientific article published in November 2009

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

scientific article

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

scientific article

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

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

Parallel synthesis and anti-malarial activity of a sulfonamide library.

scientific article

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

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

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 antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives.

scientific article

Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

scientific article published on February 2003

Synthesis of a 200-member library of squaric acid N-hydroxylamide amides

scientific article

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

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

scientific article

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

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

article published in 2013

List of works by Rébecca F Déprez-Poulain

1,4-bis(3-aminopropyl)piperazine libraries: from the discovery of classical chloroquine-like antimalarials to the identification of new targets.

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

A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues

ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion

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

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

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

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.

Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors.

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

Ensemble cryoEM elucidates the mechanism of insulin capture and degradation by human insulin degrading enzyme

Facts, figures and trends in lead generation

Hydroxamates: relationships between structure and plasma stability

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

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

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

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.

Parallel synthesis and anti-malarial activity of a sulfonamide library.

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

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

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 antimalarial evaluation of new 1,4-bis(3-aminopropyl)piperazine derivatives.

Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

Synthesis of a 200-member library of squaric acid N-hydroxylamide amides

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

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

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

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