title: Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
abstract: Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. liangqin_guo@merck.com
authors.forename: Liangqin
authors.initials: L
authors.lastname: Guo
authors.forename: Zhixiong
authors.initials: Z
authors.lastname: Ye
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
authors.forename: Shuwen
authors.initials: S
authors.lastname: He
authors.forename: Raman K
authors.initials: RK
authors.lastname: Bakshi
authors.forename: Iyassu K
authors.initials: IK
authors.lastname: Sebhat
authors.forename: Peter H
authors.initials: PH
authors.lastname: Dobbelaar
authors.forename: Qingmei
authors.initials: Q
authors.lastname: Hong
authors.forename: Tianying
authors.initials: T
authors.lastname: Jian
authors.forename: James P
authors.initials: JP
authors.lastname: Dellureficio
authors.forename: Nancy N
authors.initials: NN
authors.lastname: Tsou
authors.forename: Richard G
authors.initials: RG
authors.lastname: Ball
authors.forename: David H
authors.initials: DH
authors.lastname: Weinberg
authors.forename: Tanya
authors.initials: T
authors.lastname: MacNeil
authors.forename: Rui
authors.initials: R
authors.lastname: Tang
authors.forename: Constantin
authors.initials: C
authors.lastname: Tamvakopoulos
authors.forename: Qianping
authors.initials: Q
authors.lastname: Peng
authors.forename: Howard Y
authors.initials: HY
authors.lastname: Chen
authors.forename: Airu S
authors.initials: AS
authors.lastname: Chen
authors.forename: William J
authors.initials: WJ
authors.lastname: Martin
authors.forename: D Euan
authors.initials: DE
authors.lastname: MacIntyre
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001921:Brain / Q000378:metabolism; D018360:Crystallography, X-Ray; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008968:Molecular Conformation; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism; D013141:Spiro Compounds / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D010880:Piperidines; D044105:Receptor, Melanocortin, Type 4; D013141:Spiro Compounds; C032727:piperidine