Studies on the Structure-Activity Relationship of the Basic Amine of Phenylpiperazines as Melanocortin-4 Receptor Antagonists

Author(s): Chen Chen, Joe A. Tran, Melissa Arellano, Beth A. Fleck, Joseph Pontillo, Dragan Marinkovic, Fabio C. Tucci, Jenny Wen, John Saunders.

Journal Name: Medicinal Chemistry

Volume 4 , Issue 1 , 2008

Abstract:

A series of piperazinephenethylamines were synthesized to study the contribution of a basic amine to binding affinity at the melanocortin-4 receptor. Several potent compounds from this series possessed subnanomolar Ki values in a competition binding assay.

Keywords: Melanocortin-4 receptor, antagonist, piperazinephenethylamine, synthesis

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Article Details

VOLUME: 4
ISSUE: 1
Year: 2008
Page: [67 - 74]
Pages: 8
DOI: 10.2174/157340608783331498

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