Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor

Author(s): Fabio C. Tucci, Joe A. Tran, Wanlong Jiang, Joseph Pontillo, Dragan Marinkovic, Nicole S. White, Melissa Arellano, Beth A. Fleck, Jenny Wen, John Saunders, Alan C. Foster, Chen Chen.

Abstract:

A series of piperazinephen-1-ylehtylamines were synthesized and evaluated for their biological activity at the human melanocortin-4 receptor. This modification reduced the size and flexibility of the N-alkyl side-chain of some earlier lead compounds, while maintained the low nanomolar binding affinity.

Keywords: Melanocortin, antagonist, piperazinephenylamine, synthesis

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Article Details

VOLUME: 3
ISSUE: 5
Year: 2006
Page: [311 - 315]
Pages: 5
DOI: 10.2174/157018006777574249
Price: $58