Structure-activity studies on a 1,2,3-triazole derivative, a potent in vitro inhibitor of prostaglandin synthesis: the role of the heterocyclic ring.
This paper reports further structural modifications concerning the 1,2,3-triazole ring of the compound A, an effective in vitro inhibitor of prostaglandin synthesis. The introduction of different heterocyclic rings provided further information about of the role of the heterocyclic ring in enzymatic inhibition, as regards the number and position of the nitrogen atoms, the electronic effects, basicity, steric hindrance and hydrophilicity. The benzimidazole derivative 4e proved to possess a high enzymatic inhibitory activity.
Biagi
G
G
Istituto di Chimica Farmaceutica e Tossicologica, Università di Pisa, Italy.
Dell'Omodarme
G
G
Ferretti
M
M
Giorgi
I
I
Livi
O
O
Scartoni
V
V
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D011448:Prostaglandin Antagonists; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D016861:Cyclooxygenase Inhibitors; D006571:Heterocyclic Compounds; D011448:Prostaglandin Antagonists; D014230:Triazoles