Discovery, synthesis and biological evaluation of novel glucokinase activators

Autor:	Peter William Rodney Caulkett, Scott Boyd, Clifford David Jones, Gordon S. Currie, Sarah Lackie, Emma Grange, Craig Johnstone, Barry R. Hayter, Harold Gaskin, Christopher D. Davies, Darren Mckerrecher, Rod B. Hargreaves, Mark L. Fenwick, Roger James, Rayner John Wall, Keith M. Johnson, Joanne V. Allen, Rolf Peter Walker, Suzanne S. Bowker
Rok vydání:	2005
Předmět:	Clinical Biochemistry Drug Evaluation Preclinical Enzyme Activators Pharmaceutical Science Biochemistry Chemical synthesis In vivo Glucokinase Drug Discovery Animals Rats Wistar Kinase activator Molecular Biology Biological evaluation Activator (genetics) Chemistry Organic Chemistry Biological activity Rats Enzyme Activation Thiazoles Lipophilicity Molecular Medicine Female
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:2103-2106
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2005.01.087
Popis:	The identification, synthesis and SAR of a novel series of glucokinase activators is described. The interplay between lipophilicity, potency and physical properties is discussed, and compound 22 highlighted as having a suitable balance. In vivo pharmacokinetic and acute efficacy studies on this compound are also presented.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06fc478426effd07bc452f839f361110 https://doi.org/10.1016/j.bmcl.2005.01.087 Zobrazit plný text záznamu Full Text from ScienceDirect