An 1,2,3-triazole derivative bioisoster of a potent in vitro prostaglandin synthesis inhibitor: preparation and biological activity

G Biagi; G Dell'Omodarme; I Giorgi; O Livi; V Scartoni; V Di Bussolo

An 1,2,3-triazole derivative bioisoster of a potent in vitro prostaglandin synthesis inhibitor: preparation and biological activity

Farmaco. 1992 Jan;47(1):91-8.

Authors

G Biagi¹, G Dell'Omodarme, I Giorgi, O Livi, V Scartoni, V Di Bussolo

Affiliation

¹ Istituto di Chimica Farmaceutica e Tossicologica, Università di Pisa.

PMID: 1616580

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Inflammatory Agents, Non-Steroidal / pharmacology
Aspirin / pharmacology
Cyclooxygenase Inhibitors / chemical synthesis*
Cyclooxygenase Inhibitors / pharmacology
Humans
In Vitro Techniques
Indomethacin / pharmacology
Malondialdehyde / metabolism
Prostaglandin Antagonists
Triazoles / chemical synthesis*
Triazoles / pharmacology

Substances

Anti-Inflammatory Agents, Non-Steroidal
Cyclooxygenase Inhibitors
Prostaglandin Antagonists
Triazoles
Malondialdehyde
Aspirin
Indomethacin