title: Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
abstract: The design and synthesis of a series of potent 1,3,4-trisubstituted-2-oxopiperazine based MC4 agonists are described. The tripeptidomimetic analogs (12a,b and 23) and the dipeptidomimetic 27 displayed single-nanomolar binding affinity and agonist potency for MC4R and excellent selectivity for MC4R relative to MC1R.
authors.affiliation: Procter & Gamble Pharmaceuticals, Health Care Research Center, Mason, OH 45040, USA. tian.x@hotmail.com
authors.forename: Xinrong
authors.initials: X
authors.lastname: Tian
authors.forename: Rajesh K
authors.initials: RK
authors.lastname: Mishra
authors.forename: Adrian G
authors.initials: AG
authors.lastname: Switzer
authors.forename: X Eric
authors.initials: XE
authors.lastname: Hu
authors.forename: Nick
authors.initials: N
authors.lastname: Kim
authors.forename: Adam W
authors.initials: AW
authors.lastname: Mazur
authors.forename: Frank H
authors.initials: FH
authors.lastname: Ebetino
authors.forename: John A
authors.initials: JA
authors.lastname: Wos
authors.forename: Doreen
authors.initials: D
authors.lastname: Crossdoersen
authors.forename: Beth B
authors.initials: BB
authors.lastname: Pinney
authors.forename: Julie A
authors.initials: JA
authors.lastname: Farmer
authors.forename: Russell J
authors.initials: RJ
authors.lastname: Sheldon
mesh_terms: D015195:Drug Design; D006146:Guanidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D006146:Guanidines; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4