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Bioorg Med Chem. 2007 Aug 1;15(15):5166-76. Epub 2007 May 17.

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.

Author information

1
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.

PMID:
17544282
DOI:
10.1016/j.bmc.2007.05.026
[Indexed for MEDLINE]

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