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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 |

REPOSITORIES: biostudies-literature

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