| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365707 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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 Ki of 0.94Â nM in binding and IC50 of 21Â nM in functional activity. 12a also demonstrated efficacy in a mouse cachexia model.
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Authors
Wanlong Jiang, 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,