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Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity |
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| Authors: | Tran Joe A Tucci Fabio C Jiang Wanlong Marinkovic Dragan Chen Caroline W Arellano Melissa Markison Stacy Fleck Beth A Wen Jenny White Nicole S Pontillo Joseph Saunders John Marks Daniel Hoare Sam R Madan Ajay Foster Alan C Chen Chen |
| Institution: | Department of Medicinal Chemistry, Neurocrine Biosciences Inc, San Diego, CA 92130, USA. |
| Abstract: | A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good oral bioavailabilities. In addition, 12e demonstrated in vivo efficacy in a murine cachexia model. |
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