Design of a series of bicyclic HIV-1 integrase inhibitors. Part 2: Azoles: Effective metal chelators

Autor:	John Deadman, Eric Dale Jones, David Ian Rhodes, Changjiang Yu, Nick Vandegraaff, Jonathan Coates, Xinming Li, Xiao Feng, Giang Thanh Le, Lisa Jane Winfield, Long Lu, Neeranat Thienthong
Rok vydání:	2010
Předmět:	Azoles Stereochemistry Isostere Clinical Biochemistry Pharmaceutical Science Integrase inhibitor HIV Integrase Biochemistry Chemical synthesis Bridged Bicyclo Compounds Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Structure–activity relationship HIV Integrase Inhibitors Thiazole Molecular Biology Chelating Agents Oxazole biology Bicyclic molecule Organic Chemistry Integrase chemistry Metals Drug Design HIV-1 biology.protein Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 20:5909-5912
ISSN:	0960-894X
Popis:	Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3111b9931b6a6bde208784045591f40c https://doi.org/10.1016/j.bmcl.2010.07.081 Zobrazit plný text záznamu Full Text from ScienceDirect