Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377741 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
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 α-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 β-alanine was incorporated onto the benzylamine. Some compounds demonstrated good potency, moderate selectivity, and oral bioavailability.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wanlong Jiang, 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,