R. Deprez-Poulain

发表

Drug Target Engagement Using Coupled Cellular Thermal Shift Assay—Acoustic Reverse-Phase Protein Array

F. Leroux, B. Déprez, C. Couturier, 2019, SLAS discovery : advancing life sciences R & D.

Natural Compounds: Leads or Ideas? Bioinspired Molecules for Drug Discovery

Rebecca Deprez-Poulain, Benoit Deprez, B. Déprez, 2008, Chemical biology & drug design.

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

B. Déprez, R. Deprez-Poulain, D. Bosc, 2016, Future medicinal chemistry.

Insulin-Degrading Enzyme, an Under-Estimated Potential Target to Treat Cancer?

F. Leroux, B. Déprez, R. Deprez-Poulain, 2022, Cells.

Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.

Wei-Jen Tang, F. Leroux, B. Déprez, 2019, European journal of medicinal chemistry.

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

David R. Liu, Yong Zi Tan, B. Carragher, 2018, eLife.

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

P. van Endert, G. Lippens, Wei-Jen Tang, 2015, Nature Communications.

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

B. Déprez, R. Deprez-Poulain, Julie Charton, 2012 .

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

G. Laconde, B. Déprez, R. Deprez-Poulain, 2010 .

ADAMTS5 promotes murine adipogenesis and visceral adipose tissue expansion

I. Scroyen, D. Bauters, H. Lijnen, 2016, Thrombosis and Haemostasis.

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

F. Leroux, J. Dumont, B. Déprez, 2014, Future medicinal chemistry.

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

P. Renard, F. Leroux, B. Déprez, 2017, Journal of medicinal chemistry.

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

B. Villoutreix, O. Sperandio, F. Leroux, 2010, Bioorganic & medicinal chemistry letters.

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.

B. Déprez, N. Willand, R. Deprez-Poulain, 2011, European journal of medicinal chemistry.

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

B. Déprez, R. Deprez-Poulain, Marion Flipo, 2007, Bioorganic & medicinal chemistry.

Solvent-free microwave-assisted Meyers’ lactamization

P. Roussel, G. Laconde, B. Déprez, 2010 .

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

G. Laconde, B. Déprez, R. Deprez-Poulain, 2012 .

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

G. Laconde, B. Déprez, N. Willand, 2011 .

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

G. Laconde, B. Déprez, N. Willand, 2013 .

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

G. Laconde, B. Déprez, R. Deprez-Poulain, 2010 .

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

C. Sergheraert, L. Maes, P. Grellier, 2003, Journal of medicinal chemistry.

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

F. Leroux, J. Dumont, B. Déprez, 2012 .

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

B. Déprez, R. Deprez-Poulain, Xiaoan Wen, 2012 .

Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines.

C. Sergheraert, J. Leger, C. Jarry, 2004, Journal of medicinal chemistry.

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

B. Villoutreix, O. Sperandio, Gaëlle Deglane, 2013, European journal of medicinal chemistry.

Fast and efficient solvent-free Passerini reaction

Till Bousquet, R. Deprez-Poulain, F. Agbossou-Niedercorn, 2012 .

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

G. Laconde, B. Déprez, R. Deprez-Poulain, 2012 .

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

B. Staels, A. Tailleux, B. Déprez, 2009, Bioorganic & medicinal chemistry letters.

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.

B. Déprez, N. Willand, R. Deprez-Poulain, 2012 .

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

C. Sergheraert, P. Grellier, R. Deprez-Poulain, 2003, Bioorganic & medicinal chemistry letters.

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

C. Sergheraert, P. Grellier, R. Deprez-Poulain, 2003, Bioorganic & medicinal chemistry letters.

Convenient synthesis of 4H-1,2,4-triazole-3-thiols using di-2-pyridylthionocarbonate

B. Déprez, R. Deprez-Poulain, Julie Charton, 2007 .

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

Wei-Jen Tang, B. Staels, F. Leroux, 2015, European journal of medicinal chemistry.

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

L. Buée, Wei-Jen Tang, O. Sperandio, 2014, European journal of medicinal chemistry.

Kinetic Target-Guided Synthesis: reaching the age of maturity.

B. Déprez, R. Deprez-Poulain, O. Castillo-Aguilera, 2019, Journal of medicinal chemistry.

Synthetic EthR inhibitors boost antituberculous activity of ethionamide

Amit Singhal, Marc Aumercier, Florence Leroux, 2009, Nature Medicine.

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

F. Leroux, B. Déprez, R. Deprez-Poulain, 2008, Bioorganic & medicinal chemistry letters.

Optimization of 1,2,4-Triazole-3-thiones toward Broad-Spectrum Metallo-β-lactamase Inhibitors Showing Potent Synergistic Activity on VIM- and NDM-1-Producing Clinical Isolates.

S. Mangani, G. Feller, Filippo Vascon, 2022, Journal of medicinal chemistry.

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

E. Saridakis, D. Vourloumis, R. Deprez-Poulain, 2017, ACS medicinal chemistry letters.

Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry

F. Leroux, B. Déprez, N. Willand, 2021, Molecules.

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

B. Déprez, N. Willand, R. Deprez-Poulain, 2007 .

Hydroxamates: relationships between structure and plasma stability.

B. Déprez, R. Deprez-Poulain, Marion Flipo, 2009, Journal of medicinal chemistry.

Efficient Propylphosphonic Anhydride (®T3P) Mediated Synthesis of Benzothiazoles, Benzoxazoles and Benzimidazoles.

B. Déprez, R. Deprez-Poulain, Xiaoan Wen, 2012 .

Identification of indole-based activators of insulin degrading enzyme.

B. Staels, F. Leroux, B. Déprez, 2021, European journal of medicinal chemistry.

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

L. Maes, F. Leroux, B. Déprez, 2012, Journal of medicinal chemistry.

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

B. Déprez, R. Deprez-Poulain, I. Florent, 2007, Journal of medicinal chemistry.

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

P. Melnyk, R. Deprez-Poulain, 2005, Combinatorial chemistry & high throughput screening.

Frontiers in Medicinal Chemistry

S. A. Hutchinson, H. Wolfson, R. Nussinov, 2016 .

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

David R. Liu, Yong Zi Tan, B. Carragher, 2018, eLife.

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

C. Sergheraert, P. Grellier, R. Deprez-Poulain, 2003, Bioorganic & medicinal chemistry letters.

Discovery, Structure-Activity Relationships, and In Vivo Activity of Dihydropyridone Agonists of the Bile Acid Receptor TGR5.

B. Villoutreix, P. Roussel, B. Staels, 2023, Journal of Medicinal Chemistry.

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

B. Déprez, R. Deprez-Poulain, Julie Charton, 2008, Combinatorial chemistry & high throughput screening.

Multi-component reaction for the preparation of 1,5-disubstituted 1,2,3-triazoles by in-situ generation of azides and nickel-catalyzed azide-alkyne cycloaddition

B. Déprez, R. Deprez-Poulain, D. Bosc, 2021, Tetrahedron Letters.