title: Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
abstract: Design, syntheses and structure-activity relationships of N-acetylated piperazine privileged structures containing MC4R agonist compounds were described. The most potent derivatives were low nM MC4R selective full agonists. Several compounds from the series had modest pharmacokinetic properties.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. qingmei_hong@merck.com
authors.forename: Qingmei
authors.initials: Q
authors.lastname: Hong
authors.forename: Raman K
authors.initials: RK
authors.lastname: Bakshi
authors.forename: James
authors.initials: J
authors.lastname: Dellureficio
authors.forename: Shuwen
authors.initials: S
authors.lastname: He
authors.forename: Zhixiong
authors.initials: Z
authors.lastname: Ye
authors.forename: Peter H
authors.initials: PH
authors.lastname: Dobbelaar
authors.forename: Iyassu K
authors.initials: IK
authors.lastname: Sebhat
authors.forename: Liangqin
authors.initials: L
authors.lastname: Guo
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
authors.forename: Tianying
authors.initials: T
authors.lastname: Jian
authors.forename: Rui
authors.initials: R
authors.lastname: Tang
authors.forename: Rubana N
authors.initials: RN
authors.lastname: Kalyani
authors.forename: Tanya
authors.initials: T
authors.lastname: Macneil
authors.forename: Aurawan
authors.initials: A
authors.lastname: Vongs
authors.forename: Charles I
authors.initials: CI
authors.lastname: Rosenblum
authors.forename: David H
authors.initials: DH
authors.lastname: Weinberg
authors.forename: Qingping
authors.initials: Q
authors.lastname: Peng
authors.forename: Constantin
authors.initials: C
authors.lastname: Tamvakopoulos
authors.forename: Randy R
authors.initials: RR
authors.lastname: Miller
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Stearns
authors.forename: Doreen
authors.initials: D
authors.lastname: Cashen
authors.forename: Willian J
authors.initials: WJ
authors.lastname: Martin
authors.forename: Airu S
authors.initials: AS
authors.lastname: Chen
authors.forename: Joseph M
authors.initials: JM
authors.lastname: Metzger
authors.forename: Howard Y
authors.initials: HY
authors.lastname: Chen
authors.forename: Allison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Euan
authors.initials: E
authors.lastname: Maclntyre
authors.forename: Lex H T
authors.initials: LH
authors.lastname: Van der Ploeg
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000818:Animals; D006801:Humans; D008024:Ligands; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D008024:Ligands; D010879:Piperazines; D044105:Receptor, Melanocortin, Type 4; D000077489:Piperazine