Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2803-6. doi: 10.1016/j.bmcl.2012.02.072.
Masahide Odan  1 ,  Natsuki Ishizuka ,  Yoshiharu Hiramatsu ,  Masanao Inagaki ,  Hiroshi Hashizume ,  Yasuhiko Fujii ,  Susumu Mitsumori ,  Yasuhide Morioka ,  Masahiko Soga ,  Masashi Deguchi ,  Kiyoshi Yasui ,  Akinori Arimura
Affiliations
  • 1. Shionogi Pharmaceutical Research Center, Shionogi & Co., Ltd 1-1, Toyonaka, Osaka, Japan. [email protected]
PMID: 22444677 DOI: 10.1016/j.bmcl.2012.02.072
Abstract

The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure-activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).

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