title: Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
abstract: Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christina_madsen_duggan@merck.com
authors.forename: Christina B
authors.initials: CB
authors.lastname: Madsen-Duggan
authors.forename: John S
authors.initials: JS
authors.lastname: Debenham
authors.forename: Thomas F
authors.initials: TF
authors.lastname: Walsh
authors.forename: Richard B
authors.initials: RB
authors.lastname: Toupence
authors.forename: Song X
authors.initials: SX
authors.lastname: Huang
authors.forename: Junying
authors.initials: J
authors.lastname: Wang
authors.forename: Xinchun
authors.initials: X
authors.lastname: Tong
authors.forename: Julie
authors.initials: J
authors.lastname: Lao
authors.forename: Tung M
authors.initials: TM
authors.lastname: Fong
authors.forename: Marie-Therese
authors.initials: MT
authors.lastname: Schaeffer
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: 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: D Euan
authors.initials: DE
authors.lastname: MacIntyre
authors.forename: Lex H T
authors.initials: LH
authors.lastname: Van der Ploeg
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005247:Feeding Behavior / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D008968:Molecular Conformation; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists*; D013329:Structure-Activity Relationship; D013696:Temperature; D014050:Toluene / Q000737:chemistry
chemical_list: D011725:Pyridines; D043884:Receptor, Cannabinoid, CB1; D014050:Toluene