1426151-84-9Relevant academic research and scientific papers
Trisubstituted sulfonamides: A new chemotype for development of potent and selective CB2 receptor inverse agonists
Ouyang, Qin,Tong, Qin,Feng, Rentian,Myint, Kyaw-Zeyar,Yang, Peng,Xie, Xiang-Qun
, p. 387 - 392 (2013/06/26)
An extensive exploration of the structure-activity relationship of a trisubstituted sulfonamide series led to the identification of 39, which is a potent and selective CB2 receptor inverse agonist [K i(CB2) = 5.4 nM, and Ki(CB1) = 500 nM]. The functional properties measured by cAMP assays indicated that the selected compounds were CB2 inverse agonists with high potency values (for 34, EC50 = 8.2 nM, and for 39, EC50 = 2.5 nM). Furthermore, an osteoclastogenesis bioassay indicated that trisubstituted sulfonamide compounds showed great inhibition of osteoclast formation.
