Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists

…, R Emkey, RT Fremeau Jr, JC Harmange…

Index: Cheng, Yuan; Albrecht, Brian K.; Brown, James; Buchanan, John L.; Buckner, William H.; DiMauro, Erin F.; Emkey, Renee; Fremeau Jr., Robert T.; Harmange, Jean-Christophe; Hoffman, Beth J.; Huang, Liyue; Huang, Ming; Lee, Josie Han; Lin, Fen-Fen; Martin, Matthew W.; Nguyen, Hung Q.; Patel, Vinod F.; Tomlinson, Susan A.; White, Ryan D.; Xia, Xiaoyang; Hitchcock, Stephen A. Journal of Medicinal Chemistry, 2008 , vol. 51, # 16 p. 5019 - 5034

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Citation Number: 43

Abstract

The CB2 receptor is an attractive therapeutic target for analgesic and anti-inflammatory agents. Herein we describe the discovery of a novel class of oxadiazole derivatives from which potent and selective CB2 agonist leads were developed. Initial hit 7 was identified from a cannabinoid target-biased library generated by virtual screening of sample collections using a pharmacophore model in combination with a series of ...