| Literature DB >> 16777413 |
Wanlong Jiang1, Fabio C Tucci, Caroline W Chen, Melissa Arellano, Joe A Tran, Nicole S White, Dragan Marinkovic, Joseph Pontillo, Beth A Fleck, Jenny Wen, John Saunders, Ajay Madan, Alan C Foster, Chen Chen.
Abstract
A series of 3-arylpropionylpiperazines were synthesized as antagonists of the melanocortin-4 receptor. Their potency was found to be increased by replacing the alpha-methyl substituent of the initial lead 11 with a larger s-Bu or i-Bu group. Further potency enhancement was observed when a glycine or beta-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.Entities:
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Year: 2006 PMID： 16777413 DOI： 10.1016/j.bmcl.2006.05.088
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823