Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors

Autor:	Jean-Marie Genevard, Vanida Vongsouthi, M. Busemann, K. Wolf, G. Le Fralliec, A. Aschenbrenner, Alexis Denis, Vincent Gerusz, Chrystelle Oliveira, Sonia Escaich, Nicolas Desroy, Stéphanie Floquet, François Moreau
Rok vydání:	2008
Předmět:	Heptosyltransferase Antivirulence Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Microbial Sensitivity Tests Crystallography X-Ray Biochemistry Models Biological Structure-Activity Relationship Anti-Infective Agents Drug Resistance Multiple Bacterial Drug Discovery Anti infectives Molecular Biology Virtual screening Binding Sites Molecular Structure Chemistry Organic Chemistry Glycosyltransferases Anti-Bacterial Agents Kinetics Models Chemical Drug Design Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 18(14)
ISSN:	1464-3405
Popis:	Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2-aryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-ones identified by virtual screening.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0f2874b0abf51160955764f15f402dc https://pubmed.ncbi.nlm.nih.gov/18571407 Zobrazit plný text záznamu Full Text from ScienceDirect