Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole.
Four new aryl-sulfonamide derivatives (3a, 4a, 5a-b), having methylenedioxy group attached to phenyl ring, were prepared from natural safrole and evaluated as anti-inflammatory agents. The N-methylsulfonamide 3a and corresponding retrosulfonamide derivative 5a were more active than standards indomethacin and nimesulide, at the same molar concentration, in carrageenan-induced pleurisy assay.
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Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Brazil.
Silva
K C
KC
Miranda
A L
AL
Fraga
C A
CA
Barreiro
E J
EJ
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D004195:Disease Models, Animal; D004341:Drug Evaluation; D004487:Edema / Q000188:drug therapy; D005260:Female; D007189:Indans / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D008297:Male; D010998:Pleurisy / Q000188:drug therapy; D051381:Rats; D012451:Safrole / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D007189:Indans; C059178:flosulide; D012451:Safrole