title: Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
abstract: A series of substituted chromones were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor 1. Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats were discovered.
authors.affiliation: Department of Medicinal Chemistry, Neurocrine Biosciences Inc., San Diego, CA 92130, USA. bdyck@neurocrine.com
authors.forename: Brian
authors.initials: B
authors.lastname: Dyck
authors.forename: Liren
authors.initials: L
authors.lastname: Zhao
authors.forename: Junko
authors.initials: J
authors.lastname: Tamiya
authors.forename: Joseph
authors.initials: J
authors.lastname: Pontillo
authors.forename: Sarah
authors.initials: S
authors.lastname: Hudson
authors.forename: Brett
authors.initials: B
authors.lastname: Ching
authors.forename: Christopher E
authors.initials: CE
authors.lastname: Heise
authors.forename: Jenny
authors.initials: J
authors.lastname: Wen
authors.forename: Christi
authors.initials: C
authors.lastname: Norton
authors.forename: Ajay
authors.initials: A
authors.lastname: Madan
authors.forename: David
authors.initials: D
authors.lastname: Schwarz
authors.forename: Warren
authors.initials: W
authors.lastname: Wade
authors.forename: Val S
authors.initials: VS
authors.lastname: Goodfellow
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002867:Chromones / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D008543:Melanins / Q000737:chemistry*; D008862:Microsomes, Liver / Q000378:metabolism; D008956:Models, Chemical; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry; D051381:Rats; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013997:Time Factors
chemical_list: D002867:Chromones; D008543:Melanins; D015363:Quinolones; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor