Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists
作者:Anil Vasudevan、Andrew J. Souers、Jennifer C. Freeman、Mary K. Verzal、Ju Gao、Mathew M. Mulhern、Derek Wodka、John K. Lynch、Kenneth M. Engstrom、Seble H. Wagaw、Sevan Brodjian、Brian Dayton、Doug H. Falls、Eugene Bush、Michael Brune、Robin D. Shapiro、Kennan C. Marsh、Lisa E. Hernandez、Christine A. Collins、Philip R. Kym
DOI:10.1016/j.bmcl.2005.08.049
日期:2005.12
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice. (c) 2005 Published by Elsevier Ltd.