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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 3, Issue 5, 2006

Page: [311 - 315] Pages: 5

DOI: 10.2174/157018006777574249

Price: $65


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.

Keywords: Melanocortin, antagonist, piperazinephenylamine, synthesis

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