title: Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
abstract: Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB1R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good pharmacokinetic and brain levels, but was modestly active in blocking CB1R agonist-mediated hypothermia.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: Helen E
authors.initials: HE
authors.lastname: Armstrong
authors.forename: Amy
authors.initials: A
authors.lastname: Galka
authors.forename: Linus S
authors.initials: LS
authors.lastname: Lin
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Lanza
authors.forename: James P
authors.initials: JP
authors.lastname: Jewell
authors.forename: Shrenik K
authors.initials: SK
authors.lastname: Shah
authors.forename: Ravi
authors.initials: R
authors.lastname: Guthikonda
authors.forename: Quang
authors.initials: Q
authors.lastname: Truong
authors.forename: Linda L
authors.initials: LL
authors.lastname: Chang
authors.forename: Grace
authors.initials: G
authors.lastname: Quaker
authors.forename: Vincent J
authors.initials: VJ
authors.lastname: Colandrea
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Junying
authors.initials: J
authors.lastname: Wang
authors.forename: Sherry
authors.initials: S
authors.lastname: Xu
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Chun-Pyn
authors.initials: CP
authors.lastname: Shen
authors.forename: Julie
authors.initials: J
authors.lastname: Lao
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Lauren P
authors.initials: LP
authors.lastname: Shearman
authors.forename: D Sloan
authors.initials: DS
authors.lastname: Stribling
authors.forename: Kimberly
authors.initials: K
authors.lastname: Rosko
authors.forename: Alison
authors.initials: A
authors.lastname: Strack
authors.forename: Sookhee
authors.initials: S
authors.lastname: Ha
authors.forename: Lex
authors.initials: L
authors.lastname: Van der Ploeg
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
authors.forename: William K
authors.initials: WK
authors.lastname: Hagmann
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001923:Brain Chemistry; D063385:Cannabinoid Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007035:Hypothermia / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D010599:Pharmacokinetics; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D019440:Anti-Obesity Agents; D063385:Cannabinoid Receptor Modulators; D043884:Receptor, Cannabinoid, CB1; D013449:Sulfonamides