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Bioorg Med Chem Lett. 2009 Feb 1;19(3):976-80. doi: 10.1016/j.bmcl.2008.11.085. Epub 2008 Nov 27.

Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes: 1. Identification of 1-amino-1-cycloalkyl carboxylic acid headgroups.

Author information

1
Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, USA. steven.m.sparks@gsk.com

Abstract

Optimization of the amino acid residue within a series of anthranilimide-based glycogen phosphorylase inhibitors is described. These studies culminated in the identification of anthranilimides 16 and 22 which displayed potent in vitro inhibition of GPa in addition to reduced inhibition of CYP2C9 and excellent pharmacokinetic properties.

PMID:
19095442
DOI:
10.1016/j.bmcl.2008.11.085
[Indexed for MEDLINE]

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