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

Chen      Chen; Joe   A.   Tran; Melissa      Arellano; Beth   A.   Fleck; Joseph      Pontillo; Dragan      Marinkovic; Fabio   C.   Tucci; Jenny      Wen; John      Saunders

Medicinal Chemistry

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

DOI: 10.2174/157340608783331498

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

Page: [67 - 74] Pages: 8

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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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