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

doi:10.2174/157340608783331498

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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Medicinal Chemistry

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

Volume: 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

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

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.

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Chen Chen, Tran A. Joe, Arellano Melissa, Fleck A. Beth, Pontillo Joseph, Marinkovic Dragan, Tucci C. Fabio, Wen Jenny and Saunders John, Studies on the Structure-Activity Relationship of the Basic Amine of Phenylpiperazines as Melanocortin-4 Receptor Antagonists, Medicinal Chemistry 2008; 4 (1) . https://dx.doi.org/10.2174/157340608783331498