| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376060 | Bioorganic & Medicinal Chemistry Letters | 2007 | 7 Pages |
Abstract
A series of trans-N-alkyl-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanemethylamines was synthesized and characterized for binding and function at the melanocortin-4 receptor (MC4R), and several potent benzylamine derivatives were identified. Compound 18v was found to bind MC4R with potent affinity (Ki = 0.5 nM) and high selectivity over the other melanocortin subtypes and behaved as a functional antagonist (IC50 = 48 nM).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Caroline W. Chen, Joe A. Tran, Beth A. Fleck, Fabio C. Tucci, Wanlong Jiang, Chen Chen,