4-Benzoyl- and 4-benzyl-1,2,3-triazol-N-acetic acids, in vitro inhibitors of the prostaglandin synthesis.
Several 4-benzoyl- and 4-benzyl-1,2,3-triazol-N-acetic derivatives were synthesized and tested. The compounds were prepared by nucleophilic substitution, 1,3-dipolar cycloaddition and usual functional group conversion reactions. Numerous derivatives were evaluated in vitro for their ability to inhibit the prostaglandin synthesis and to displace labelled [14C]indomethacin from bovine vesicular gland microsomes. Some compounds showed biological activity.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D001667:Binding, Competitive; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D005088:Exocrine Glands / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D007213:Indomethacin / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D011448:Prostaglandin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D011453:Prostaglandins / Q000096:biosynthesis*; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D001593:Benzyl Compounds; D011448:Prostaglandin Antagonists; D011453:Prostaglandins; D014230:Triazoles; D007213:Indomethacin