Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. Academic Article uri icon


  • In order to create novel analgesic agents without gastric disturbance, structurally simple cyclooxygenase-1 (COX-1) inhibitors with a benzenesulfonanilide skeleton were designed and synthesized. As a result, compounds 11f and 15a, which possess a p-amino group on the benzenesulfonyl moiety and p-chloro group on the anilino moiety, showed COX-1-selective inhibition. Moreover compound 11f, which is the most potent compound in this study showed more potent analgesic activity than that of aspirin at 30 mg/kg by po. The anti-inflammatory activity and gastric damage, however, were very weak or not detectably different from aspirin. Since the structure of our COX-1 inhibitors are very simple, they may be useful as lead compounds for superior COX-1 inhibitors as analgesic agents without gastric disturbance.

published proceedings

  • Bioorg Med Chem

altmetric score

  • 9

author list (cited authors)

  • Zheng, X., Oda, H., Takamatsu, K., Sugimoto, Y., Tai, A., Akaho, E., ... Sasaki, K.

citation count

  • 25

complete list of authors

  • Zheng, Xiaoxia||Oda, Hiroyuki||Takamatsu, Kayo||Sugimoto, Yukio||Tai, Akihiro||Akaho, Eiichi||Ali, Hamed Ismail||Oshiki, Toshiyuki||Kakuta, Hiroki||Sasaki, Kenji

publication date

  • January 2007