title: Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
abstract: We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA. shuwen_he@merck.com
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: Yingjie
authors.initials: Y
authors.lastname: Lai
authors.forename: Christopher L
authors.initials: CL
authors.lastname: Franklin
authors.forename: Raman K
authors.initials: RK
authors.lastname: Bakshi
authors.forename: James P
authors.initials: JP
authors.lastname: Dellureficio
authors.forename: Qingmei
authors.initials: Q
authors.lastname: Hong
authors.forename: Nancy N
authors.initials: NN
authors.lastname: Tsou
authors.forename: Richard G
authors.initials: RG
authors.lastname: Ball
authors.forename: Doreen E
authors.initials: DE
authors.lastname: Cashen
authors.forename: William J
authors.initials: WJ
authors.lastname: Martin
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: Randy R
authors.initials: RR
authors.lastname: Miller
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Stearns
authors.forename: Howard Y
authors.initials: HY
authors.lastname: Chen
authors.forename: Airu S
authors.initials: AS
authors.lastname: Chen
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: D Euan
authors.initials: DE
authors.lastname: Macintyre
authors.forename: Matthew J
authors.initials: MJ
authors.lastname: Wyvratt
authors.forename: Ravi P
authors.initials: RP
authors.lastname: Nargund
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004285:Dogs; D007172:Erectile Dysfunction / Q000188:drug therapy*; D000882:Haplorhini; D006801:Humans; D007189:Indans / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D015394:Molecular Structure; D011485:Protein Binding; D051381:Rats; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000378:metabolism*; D013141:Spiro Compounds / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
chemical_list: D007189:Indans; D044105:Receptor, Melanocortin, Type 4; D013141:Spiro Compounds