Discovery of S-444823, a potent CB1/CB2 dual agonist as an antipruritic agent
2012
Odan, Masahide | Ishizuka, Natsuki | Hiramatsu, Yoshiharu | Inagaki, Masanao | Hashizume, Hiroshi | Fujii, Yasuhiko | Mitsumori, Susumu | Morioka, Yasuhide | Soga, Masahiko | Deguchi, Masashi | Yasui, Kiyoshi | Arimura, Akinori
The optimization of a series of 3-carbamoyl 2-pyridone derivatives as CB agonists is reported. These efforts resulted in the discovery of 3-(2-(1-(cyclohexylmethyl)-2-oxo-1,2,5,6,7,8,9,10-octahydrocycloocta[b]pyridine-3-carboxamido)thiazol-4-yl)propanoic acid (21), a potent dual CB1/CB2 agonist without CNS side effects induced by CB1 receptor activation. It exhibited strong inhibition of scratching as a 1.0% acetone solution in the pruritic model.
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