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

[ Vol. 4 , Issue. 1 ]

Author(s):

Chen Chen, Joe A. Tran, Melissa Arellano, Beth A. Fleck, Joseph Pontillo, Dragan Marinkovic, Fabio C. Tucci, Jenny Wen and John Saunders   Pages 67 - 74 ( 8 )

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

Affiliation:

Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.



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