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Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB₂ Receptor Inverse Agonists.

ABSTRACT: An extensive exploration of the SAR of a trisubstituted sulfonamides series led to the identification of 39, which is a potent and selective CB₂ receptor inverse agonist (CB₂Ki = 5.4 nM, and CB₁Ki = 500 nM). The functional properties measured by cAMP assays indicated that the selected compounds were CB₂ inverse agonists with high potency values (34, EC₅₀ = 8.2 nM, and 39, EC₅₀ = 2.5 nM). Furthermore, an osteoclastogenesis bioassay indicated that trisubstituted sulfonamide compounds showed great inhibition of osteoclast formation.

SUBMITTER: Ouyang Q

PROVIDER: S-EPMC3979583 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature

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Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB2 Receptor Inverse Agonists.

Ouyang Qin Q Tong Qin Q Feng Rentian R Myint Kyaw-Zeyar KZ Yang Peng P Xie Xiang-Qun XQ

ACS medicinal chemistry letters 20130401 4

An extensive exploration of the SAR of a trisubstituted sulfonamides series led to the identification of 39, which is a potent and selective CB2 receptor inverse agonist (CB2Ki = 5.4 nM, and CB1Ki = 500 nM). The functional properties measured by cAMP assays indicated that the selected compounds were CB2 inverse agonists with high potency values (34, EC50 = 8.2 nM, and 39, EC50 = 2.5 nM). Furtherm ...[more]

PMID: 24729834

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