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Bioorg Med Chem Lett. 2007 Oct 15;17(20):5610-3. Epub 2007 Aug 23.

Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.

Author information

1
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.

PMID:
17822895
DOI:
10.1016/j.bmcl.2007.07.097
[Indexed for MEDLINE]

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