Abstract:
: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.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Zheng X,Oda H,Takamatsu K,Sugimoto Y,Tai A,Akaho E,Ali HI,Oshiki T,Kakuta H,Sasaki Kdoi
10.1016/j.bmc.2006.10.029subject
Has Abstractpub_date
2007-01-15 00:00:00pages
1014-21issue
2eissn
0968-0896issn
1464-3391pii
S0968-0896(06)00859-5journal_volume
15pub_type
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