title: Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles.
abstract: A series of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles were synthesized regioselectively using click chemistry and evaluated at CB1 cannabinoid receptors. The n-propyl ester 11 (K(i)=4.6 nM) and phenyl ester 14 (K(i)=11 nM) exhibited the most potent affinity of the series.
authors.affiliation: Department of Chemistry, University of New Orleans, 2000 Lakeshore Drive, New Orleans, LA 70148, USA.
authors.forename: Hong
authors.initials: H
authors.lastname: Shu
authors.forename: Sari
authors.initials: S
authors.lastname: Izenwasser
authors.forename: Dean
authors.initials: D
authors.lastname: Wade
authors.forename: Edwin D
authors.initials: ED
authors.lastname: Stevens
authors.forename: Mark L
authors.initials: ML
authors.lastname: Trudell
mesh_terms: D002490:Central Nervous System / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004952:Esters; D005786:Gene Expression Regulation; D006801:Humans; D007700:Kinetics; D008024:Ligands; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D011485:Protein Binding; D011720:Pyrazoles / Q000737:chemistry; D043884:Receptor, Cannabinoid, CB1 / Q000378:metabolism*; D014230:Triazoles / Q000037:antagonists & inhibitors* / Q000138:chemical synthesis*
chemical_list: D004952:Esters; D008024:Ligands; D011720:Pyrazoles; D043884:Receptor, Cannabinoid, CB1; D014230:Triazoles