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
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
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.
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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
DOI https://dx.doi.org/10.2174/157340608783331498 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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