| Literature DB >> 17822895 |
Wanlong Jiang1, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen, Stacy Markison, Dragan Marinkovic, Caroline W Chen, Melissa Arellano, Sam R Hoare, Michael Johns, Alan C Foster, John Saunders, Chen Chen.
Abstract
A series of pyrrolidinones derived from phenylalaninepiperazines were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor. In addition to their high binding affinities, these compounds displayed high functional potencies. 12a had a K(i) of 0.94 nM in binding and IC(50) of 21 nM in functional activity. 12a also demonstrated efficacy in a mouse cachexia model.Entities:
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Year: 2007 PMID： 17822895 DOI： 10.1016/j.bmcl.2007.07.097
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823