Studies on 1,2,3-triazole derivatives as in vitro inhibitors of prostaglandin synthesis.
This paper reports some new structural modifications (branching and lengthening of alkanoic substituent, increase of heterocycle-carboxylate distance) on 1,2,3-triazole derivative 1, a potent in vitro inhibitor of prostaglandin synthesis, and their influence on enzyme activity. Regarding the structural relationship between 1 and Dazoxiben, a selective thromboxane-synthetase inhibitor, the preparation and activity of some Dazoxiben analogs bearing different heterocycles, are also described.
Biagi
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Pisa.
Dell'Omodarme
G
G
Ferretti
M
M
Giorgi
I
I
Livi
O
O
Scartoni
V
V
Tiscione
E
E
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D001241:Aspirin / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007213:Indomethacin / Q000494:pharmacology; D008315:Malondialdehyde / Q000097:blood; D011448:Prostaglandin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001095:Arachidonic Acids; D011448:Prostaglandin Antagonists; D014230:Triazoles; D016718:Arachidonic Acid; D008315:Malondialdehyde; D001241:Aspirin; D007213:Indomethacin