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Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor |
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| Authors: | Jiang Wanlong Tucci Fabio C Tran Joe A Fleck Beth A Wen Jenny Markison Stacy Marinkovic Dragan Chen Caroline W Arellano Melissa Hoare Sam R Johns Michael Foster Alan C Saunders John Chen Chen |
| Affiliation: | Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. |
| 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. |
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