title: Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
abstract: The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited potent binding affinity and functional activity at MCH-R1, and good oral bioavailability in rat.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences Inc., San Diego, CA 92130, USA. mrowbottom@neurocrine.com
authors.forename: Martin W
authors.initials: MW
authors.lastname: Rowbottom
authors.forename: Troy D
authors.initials: TD
authors.lastname: Vickers
authors.forename: Brian
authors.initials: B
authors.lastname: Dyck
authors.forename: Jonathan
authors.initials: J
authors.lastname: Grey
authors.forename: Junko
authors.initials: J
authors.lastname: Tamiya
authors.forename: Mingzhu
authors.initials: M
authors.lastname: Zhang
authors.forename: Mehrak
authors.initials: M
authors.lastname: Kiankarimi
authors.forename: Dongpei
authors.initials: D
authors.lastname: Wu
authors.forename: Wesley
authors.initials: W
authors.lastname: Dwight
authors.forename: Warren S
authors.initials: WS
authors.lastname: Wade
authors.forename: David
authors.initials: D
authors.lastname: Schwarz
authors.forename: Christopher E
authors.initials: CE
authors.lastname: Heise
authors.forename: Ajay
authors.initials: A
authors.lastname: Madan
authors.forename: Andrew
authors.initials: A
authors.lastname: Fisher
authors.forename: Robert
authors.initials: R
authors.lastname: Petroski
authors.forename: Val S
authors.initials: VS
authors.lastname: Goodfellow
mesh_terms: D000818:Animals; D015394:Molecular Structure; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D011759:Pyrrolidines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor; D014508:Urea