title: Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
abstract: We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. Qingmei_hong@merck.com
authors: Qingmei
authors: Q
authors: Hong
authors: Raman K
authors: RK
authors: Bakshi
authors: Brenda L
authors: BL
authors: Palucki
authors: Min K
authors: MK
authors: Park
authors: Zhixiong
authors: Z
authors: Ye
authors: Shuwen
authors: S
authors: He
authors: Patrick G
authors: PG
authors: Pollard
authors: Iyassu K
authors: IK
authors: Sebhat
authors: Jian
authors: J
authors: Liu
authors: Liangqin
authors: L
authors: Guo
authors: Doreen E
authors: DE
authors: Cashen
authors: William J
authors: WJ
authors: Martin
authors: David H
authors: DH
authors: Weinberg
authors: Tanya
authors: T
authors: MacNeil
authors: Rui
authors: R
authors: Tang
authors: Constantin
authors: C
authors: Tamvakopoulos
authors: Qianping
authors: Q
authors: Peng
authors: Randy R
authors: RR
authors: Miller
authors: Ralph A
authors: RA
authors: Stearns
authors: Howard Y
authors: HY
authors: Chen
authors: Airu S
authors: AS
authors: Chen
authors: Alison M
authors: AM
authors: Strack
authors: Tung M
authors: TM
authors: Fong
authors: D Euan
authors: DE
authors: MacIntyre
authors: Matthew J
authors: MJ
authors: Wyvratt
authors: Ravi P
authors: RP
authors: Nargund
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004195:Disease Models, Animal; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D004435:Eating / Q000187:drug effects; D000882:Haplorhini; D051379:Mice; D009765:Obesity / Q000188:drug therapy; D010879:Piperazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use
chemical_list: D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4; D014508:Urea