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

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

Affiliation:

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.

Cite this article as:

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