Discovery, synthesis and biological evaluation of novel glucokinase activators

[Display omitted] 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 st...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 15; no. 8; pp. 2103 - 2106
Main Authors:	McKerrecher, Darren, Allen, Joanne V., Bowker, Suzanne S., Boyd, Scott, Caulkett, Peter W.R., Currie, Gordon S., Davies, Christopher D., Fenwick, Mark L., Gaskin, Harold, Grange, Emma, Hargreaves, Rod B., Hayter, Barry R., James, Roger, Johnson, Keith M., Johnstone, Craig, Jones, Clifford D., Lackie, Sarah, Rayner, John W., Walker, Rolf P.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-04-2005 Elsevier
Subjects:	Animals Biological and medical sciences Diabetes Drug Evaluation, Preclinical - methods Enzyme Activation - physiology Enzyme Activators - chemical synthesis Enzyme Activators - pharmacology Female General and cellular metabolism. Vitamins Glucokinase Glucokinase - metabolism Kinase activator Medical sciences Pharmacology. Drug treatments Rats Rats, Wistar Thiazoles - chemical synthesis Thiazoles - pharmacology Kinase activator Glucokinase Diabetes Endocrinopathy Rat Clearance Pyridine derivatives Hypoglycemic agent Activator Chemical synthesis Nicotinic acid derivatives Enzyme Transferases Acute Diabetes mellitus Rodentia Elimination Oral administration Bioavailability Physical properties Biological activity In vivo Vertebrata Mammalia Animal Benzamide derivatives Carboxamide Pharmacokinetics Lipophilicity
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Summary:	[Display omitted] 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.01.087