Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis |
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Authors: | Guo Tao Hunter Rachael C Gu Huizhong Rokosz Laura L Stauffer Tara M Hobbs Doug W |
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Institution: | Pharmacopeia Drug Discovery, Inc., P.O. Box 5350, Princeton, NJ 08543-5350, USA. tguo@pharmacop.com |
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Abstract: | -4-Amino-2-arylbutylbenzamides such as 1 were identified as micromolar MCH 1 receptor (MCH1R) antagonists via screening using a scintillation proximity assay based on 125I]-MCH binding to recombinant, human MCH1R. Subsequent lead optimization efforts using solid-phase parallel synthesis resulted in the defined structure-activity relationships and the identification of 4-amino-2-biarylbutylureas, such as 11g, as potent single digit nanomolar MCH1R antagonists. |
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