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

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

doi:10.2174/157018006777574249

ISSN: 1570-1808
E-ISSN: 1875-628X

Synthesis of Piperazinephen-1-ylethylamines as Potent and Selective Antagonists of the Human Melanocortin-4 Receptor
Authors: Fabio C. Tucci¹, Joe A. Tran², Wanlong Jiang³, Joseph Pontillo⁴, Dragan Marinkovic⁵, Nicole S. White⁶, Melissa Arellano⁷, Beth A. Fleck⁸, Jenny Wen⁹, John Saunders¹⁰, Alan C. Foster¹¹ and Chen Chen¹²
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¹ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ² Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ³ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁴ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁵ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁶ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁷ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁸ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ⁹ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ¹⁰ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ¹¹ Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA. ¹² Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Source: Letters in Drug Design & Discovery, Volume 3, Issue 5, Jul 2006, p. 311 - 315
DOI: https://doi.org/10.2174/157018006777574249
- Available online: 01 Jul 2006

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.

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2006-07-01

2025-09-07

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Article Type: Research Article

Keyword(s): antagonist; Melanocortin; piperazinephenylamine; synthesis

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

Abstract

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