title: Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
abstract: The synthesis, SAR and binding affinities of cannabinoid-1 receptor (CB1R) inverse agonists based on furo[2,3-b]pyridine scaffolds are described. Food intake, mechanism specific efficacy, pharmacokinetic, and metabolic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. john_debenham@merck.com
authors.forename: John S
authors.initials: JS
authors.lastname: Debenham
authors.forename: Christina B
authors.initials: CB
authors.lastname: Madsen-Duggan
authors.forename: Richard B
authors.initials: RB
authors.lastname: Toupence
authors.forename: Thomas F
authors.initials: TF
authors.lastname: Walsh
authors.forename: Junying
authors.initials: J
authors.lastname: Wang
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Sanjeev
authors.initials: S
authors.lastname: Kumar
authors.forename: Julie
authors.initials: J
authors.lastname: Lao
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Jing Chen
authors.initials: JC
authors.lastname: Xiao
authors.forename: Cathy R-R C
authors.initials: CR
authors.lastname: Huang
authors.forename: Chun-Pyn
authors.initials: CP
authors.lastname: Shen
authors.forename: Yue
authors.initials: Y
authors.lastname: Feng
authors.forename: Donald J
authors.initials: DJ
authors.lastname: Marsh
authors.forename: D Sloan
authors.initials: DS
authors.lastname: Stribling
authors.forename: Lauren P
authors.initials: LP
authors.lastname: Shearman
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
mesh_terms: D000818:Animals; D001578:Benzopyrans; D004285:Dogs; D015195:Drug Design; D005663:Furans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000882:Haplorhini; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D018345:Mice, Knockout; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D001578:Benzopyrans; D005663:Furans; D011725:Pyridines; D043884:Receptor, Cannabinoid, CB1; C493951:furobenzopyranone