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 , Chen Chen .

Journal Name: Letters in Drug Design & Discovery

Volume 3 , Issue 5 , 2006

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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.

Keywords: Melanocortin, antagonist, piperazinephenylamine, synthesis

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Article Details

VOLUME: 3
ISSUE: 5
Year: 2006
Page: [311 - 315]
Pages: 5
DOI: 10.2174/157018006777574249
Price: $58

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