| Literature DB >> 20933410 |
Shuwen He1, Zhixiong Ye, Peter H Dobbelaar, Raman K Bakshi, Qingmei Hong, James P Dellureficio, Iyassu K Sebhat, Liangqin Guo, Jian Liu, Tianying Jian, Yingjie Lai, Christopher L Franklin, Mikhail Reibarkh, Mark A Holmes, David H Weinberg, Tanya MacNeil, Rui Tang, Constantin Tamvakopoulos, Qianping Peng, Randy R Miller, Ralph A Stearns, Howard Y Chen, Airu S Chen, Alison M Strack, Tung M Fong, Matthew J Wyvratt, Ravi P Nargund.
Abstract
We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies led to the discovery of compound 32, which is more potent at MC4R. Compound 32 demonstrates MC4R mediated anti-obesity efficacy in rodent models.Entities:
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Year: 2010 PMID： 20933410 DOI： 10.1016/j.bmcl.2010.09.049
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823