Trisubstituted sulfonamides: a new chemotype for development of potent and selective CB2 receptor inverse agonists

Q Ouyang, Q Tong, R Feng, KZ Myint…

Index: Ouyang, Qin; Tong, Qin; Feng, Rentian; Myint, Kyaw-Zeyar; Yang, Peng; Xie, Xiang-Qun ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 4 p. 387 - 392

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Citation Number: 6

Abstract

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 K i (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 ...