Details

Autor(en) / Beteiligte

• Engler, Thomas A
• Henry, James R
• Malhotra, Sushant
• Cunningham, Brian
• Furness, Kelly
• Brozinick, Joseph
• Burkholder, Timothy P
• Clay, Michael P
• Clayton, Joshua
• Diefenbacher, Clive
• Hawkins, Eric
• Iversen, Philip W
• Li, Yihong
• Lindstrom, Terry D
• Marquart, Angela L
• McLean, Johnathan
• Mendel, David
• Misener, Elizabeth
• Briere, Daniel
• O'Toole, John C
• Porter, Warren J
• Queener, Steven
• Reel, Jon K
• Owens, Rebecca A
• Brier, Richard A
• Eessalu, Thomas E
• Wagner, Jill R
• Campbell, Robert M
• Vaughn, Renee

Titel

Substituted 3-Imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino- [6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as Highly Selective and Potent Inhibitors of Glycogen Synthase Kinase-3

Ist Teil von

• Journal of medicinal chemistry, 2004-07, Vol.47 (16), p.3934-3937

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2004

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.