Rapid and Efficient Access to Novel Bio-Inspired 3-Dimensional Tricyclic SpiroLactams as Privileged Structures via Meyers’ Lactamization

Autor: Salia Tangara, Léo Faïon, Catherine Piveteau, Frédéric Capet, Romain Godelier, Marion Michel, Marion Flipo, Benoit Deprez, Nicolas Willand, Baptiste Villemagne

Publikováno v: Pharmaceuticals, Vol 16, Iss 3, p 413 (2023)

The concept of privileged structure has been used as a fruitful approach for the discovery of novel biologically active molecules. A privileged structure is defined as a semi-rigid scaffold able to display substituents in multiple spatial directions

Externí odkaz: https://doaj.org/article/457540ee79dc4ef9b38bd6f202d0cd9c

Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases

Autor: Sushovan Dam, Salia Tangara, Claire Hamela, Theo Hattabi, Léo Faïon, Paul Carre, Rudy Antoine, Adrien Herledan, Florence Leroux, Catherine Piveteau, Maxime Eveque, Marion Flipo, Benoit Deprez, Laurent Kremer, Nicolas Willand, Baptiste Villemagne, Ruben C. Hartkoorn

Publikováno v: Journal of Medicinal Chemistry
Journal of Medicinal Chemistry, 2022, 65 (24), pp.16651-16664. ⟨10.1021/acs.jmedchem.2c01493⟩

International audience; It is critical that novel classes of antituberculosis drugs are developed to combat the increasing burden of infections by multidrug-resistant strains. To identify such a novel class of antibiotics, a chemical library of uniqu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a644599ffe66ea073b6bc501b605bcac
https://doi.org/10.1021/acs.jmedchem.2c01493

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

Autor: Cyril Couturier, Baptiste Villemagne, Florence Leroux, Damien Bosc, Nicolas Willand, Rebecca Deprez-Poulain, Benoit Deprez, Marion Flipo, Julie Charton

Publikováno v: Molecules
Molecules, Vol 26, Iss 6083, p 6083 (2021)

Chemical biology and drug discovery are two scientific activities that pursue different goals but complement each other. The former is an interventional science that aims at understanding living systems through the modulation of its molecular compone

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43cc6fa33b9749010b111d8c8c41ffac
https://pubmed.ncbi.nlm.nih.gov/34641626

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

Autor: Alexandre Wohlkonig, Florence Leroux, Nicolas Willand, Ngoc Chau Tran, Xue Li, Arnaud Machelart, Marion Flipo, Catherine Piveteau, Ruxandra Gref, René Wintjens, Martin Moune, Priscille Brodin, Baptiste Villemagne, Benoit Deprez, Alain R. Baulard

Publikováno v: ACS Infectious Diseases
ACS Infectious Diseases, American Chemical Society, 2020, 6 (3), pp.366-378. ⟨10.1021/acsinfecdis.9b00277⟩
ACS infectious diseases, 6 (3

Killing more than one million people each year, tuberculosis remains the leading cause of death from a single infectious agent. The growing threat of multidrug-resistant strains of Mycobacterium tuberculosis stresses the need for alternative therapie

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::931eaebb3f9b176f73e560ebbc8df763
https://hdl.handle.net/20.500.14017/bfe9ace9-bb59-4e70-926f-60024ea8be55

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs

Autor: Giuseppina Salzano, Ilse Manet, Priscille Brodin, Stefano Ottani, Alain R. Baulard, Jitendra Wankar, Nicolas Willand, Ruxandra Gref, Baptiste Villemagne

Publikováno v: International journal of pharmaceutics
(2017). doi:10.1016/j.ijpharm.2017.05.030
info:cnr-pdr/source/autori:Salzano, Giuseppina; Wankar, Jitendra; Ottani, Stefano; Villemagne, Baptiste; Baulard, Alain R; Willand, Nicolas; Brodin, Priscille; Manet, Ilse; Gref, Ruxandra/titolo:Cyclodextrin-based nanocarriers containing a synergic drug combination: a potential formulation for pulmonary administration of antitubercular drugs./doi:10.1016%2Fj.ijpharm.2017.05.030/rivista:International journal of pharmaceutics (Print)/anno:2017/pagina_da:/pagina_a:/intervallo_pagine:/volume

Tuberculosis (TB) remains a major global health problem. The use of ethionamide (ETH), a main second line drug, is associated to severe toxic side-effects due to its low therapeutic index. In this challenging context, "booster" molecules have been sy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9b632e351937dfa6102eae116383294
https://doi.org/10.1016/j.ijpharm.2017.05.030