An 1,2,3-triazole derivative bioisoster of a potent in vitro prostaglandin synthesis inhibitor: preparation and biological activity.
This paper reports the preparation of the triazole ester 10, a methylenic bioisoster of an oxygenated compound A, effective inhibitor of the prostaglandin synthesis in vitro. Biological evaluation of 10 and of the corresponding acid 9 shows that the compounds maintain a good enzymatic inhibitory activity compared with indomethacin and aspirin.
Biagi
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Pisa.
Dell'Omodarme
G
G
Giorgi
I
I
Livi
O
O
Scartoni
V
V
Di Bussolo
V
V
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007213:Indomethacin / Q000494:pharmacology; D008315:Malondialdehyde / Q000378:metabolism; D011448:Prostaglandin Antagonists; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D011448:Prostaglandin Antagonists; D014230:Triazoles; D008315:Malondialdehyde; D001241:Aspirin; D007213:Indomethacin