Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor

Title: Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor

Volume: 3 Issue: 5

Author(s): Fabio C. Tucci, Joe A. Tran, Wanlong Jiang, Joseph Pontillo, Dragan Marinkovic, Nicole S. White, Melissa Arellano, Beth A. Fleck, Jenny Wen, John Saunders, Alan C. Foster and Chen Chen

Affiliation:

Keywords: Melanocortin, antagonist, piperazinephenylamine, synthesis

Abstract: A series of piperazinephen-1-ylehtylamines were synthesized and evaluated for their biological activity at the human melanocortin-4 receptor. This modification reduced the size and flexibility of the N-alkyl side-chain of some earlier lead compounds, while maintained the low nanomolar binding affinity.

Cite this article as:

Tucci C. Fabio, Tran A. Joe, Jiang Wanlong, Pontillo Joseph, Marinkovic Dragan, White S. Nicole, Arellano Melissa, Fleck A. Beth, Wen Jenny, Saunders John, Foster C. Alan and Chen Chen, Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor, Letters in Drug Design & Discovery 2006; 3(5) . https://dx.doi.org/10.2174/157018006777574249