Benzenesulfonanilide-type cyclooxygenase-1-selective inhibitor
     
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Benzenesulfonanilide-type cyclooxygenase-1-selective inhibitor

4-Amino-N-(4-chlorophenyl)-N-methyl-benzenesulfonamide

Benzenesulfonanilide-type_cyclooxygenase-1-selective_inhibitor
OTAVAchemicals Catalogue Number: 7070707001
CAS Registry Number: 304913-22-2
Purity: 97%+ (HPLC)


Ref.: Zheng et al. Analgesic agents without gastric damage: Design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors. Bioorganic & Medicinal Chemistry (2007), 15, 1014-1021


Abstract: N-methyl-N-(4-chlorophenyl) 4-aminobenzenesulfonamide and N-methyl-N-(4-aminophenyl) 4-chlorobenzenesulfonamide, which possess a p-amino group on the benzenesulfonyl moiety and p-chloro group on the anilino moiety, showed COX-1-selective inhibition. Moreover, N-methyl-N-(4-chlorophenyl) 4-aminobenzenesulfonamide, 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.

 
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