In vitro inhibitors of prostaglandin synthesis: (p-thiosubstituted)-benzyl nitrogen heterocycles.
This paper reports the preparation of some (p-thiosubstituted)-benzyl (disulfides, thiols, and ethyl 2-mercaptopropionates) nitrogen heterocycles (1,2,3-triazole, imidazole, pyridine, tetrazole and 1,3,4-oxadiazole) and the evaluation of their inhibitory activity of in vitro prostaglandin synthesis. The mercaptopropionates, isosters of previously studied and very effective oxyderivatives, maintain high enzyme activity which is also present, although to a lower degree, in the corresponding disulfides.
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
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D001241:Aspirin / Q000494:pharmacology; D001593:Benzyl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008315:Malondialdehyde / Q000378:metabolism; D011448:Prostaglandin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013440:Sulfides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001095:Arachidonic Acids; D001593:Benzyl Compounds; D006571:Heterocyclic Compounds; D011448:Prostaglandin Antagonists; D013438:Sulfhydryl Compounds; D013440:Sulfides; D016718:Arachidonic Acid; D008315:Malondialdehyde; D001241:Aspirin