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Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor
Authors:Tran Joe A  Pontillo Joseph  Fleck Beth A  Marinkovic Dragan  Arellano Melissa  Tucci Fabio C  Lanier Marion  Saunders John  Jiang Wanlong  Chen Caroline W  Foster Alan C  Chen Chen
Affiliation:Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
Abstract:A series of 2-pyridinylpiperazines derived from beta-Ala-(2,4-Cl)Phe dipeptide was synthesized for the study of their SARs and possible interactions with the MC4 receptor. Compounds such as 11k (Ki=6.5 nM) possessed high potency.
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