| Literature DB >> 15267232 |
Thomas A Engler1, James R Henry, Sushant Malhotra, Brian Cunningham, Kelly Furness, Joseph Brozinick, Timothy P Burkholder, Michael P Clay, Joshua Clayton, Clive Diefenbacher, Eric Hawkins, Philip W Iversen, Yihong Li, Terry D Lindstrom, Angela L Marquart, Johnathan McLean, David Mendel, Elizabeth Misener, Daniel Briere, John C O'Toole, Warren J Porter, Steven Queener, Jon K Reel, Rebecca A Owens, Richard A Brier, Thomas E Eessalu, Jill R Wagner, Robert M Campbell, Renee Vaughn.
Abstract
Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making GSK3 an attractive target for the treatment of type 2 diabetes. Herein we report the discovery of a series of potent and selective GSK3 inhibitors. Compounds 7-12 show oral activity in an in vivo model of type II diabetes, and 9 and 12 have desirable PK properties.Entities:
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Year: 2004 PMID： 15267232 DOI： 10.1021/jm049768a
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446