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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.

Bioorganic & medicinal chemistry letters 2005 Aug 15; 15(16):3701-6

Link to PubMed abstract

Huang C CQ, Baker T T, Schwarz D D, Fan J J, Heise C CE, Zhang M M, Goodfellow V VS, Markison S S, Gogas K KR, Chen T T, Wang X XC, Zhu Y YF

Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.

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.