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ID: ALA1142773
Journal: Bioorg Med Chem Lett
Title: 1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists.
Authors: Huang CQ, Baker T, Schwarz D, Fan J, Heise CE, Zhang M, Goodfellow VS, Markison S, Gogas KR, Chen T, Wang XC, Zhu YF.
Abstract: Derivatives of 1-(4-amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine were identified as potent and functionally active MCH-R1 antagonists. One compound with Ki = 2.3 nM demonstrated good oral bioavailability (32%) and in vivo efficacy in rats.
CiteXplore: 16005225