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.
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.
authors: Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.
authors: Charles Q
authors: CQ
authors: Huang
authors: Tracy
authors: T
authors: Baker
authors: David
authors: D
authors: Schwarz
authors: Jun
authors: J
authors: Fan
authors: Christopher E
authors: CE
authors: Heise
authors: Mingzhu
authors: M
authors: Zhang
authors: Val S
authors: VS
authors: Goodfellow
authors: Stacy
authors: S
authors: Markison
authors: Kathleen R
authors: KR
authors: Gogas
authors: Takung
authors: T
authors: Chen
authors: Xiao-Chuan
authors: XC
authors: Wang
authors: Yun-Fei
authors: YF
authors: Zhu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001835:Body Weight; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008297:Male; D023421:Models, Animal; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D011759:Pyrrolidines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C491208:MCHR1 protein, rat; D011725:Pyridines; D011759:Pyrrolidines; D017481:Receptors, Somatostatin