Synthesis of some thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones and their novel Michael addition products with anti-inflammatory activities.
In this study, 21 new compounds having 2-methyl-6-benzylidenethiazolo[3,2-b]-1,2,4-triazol-5(6H)-one (2-4) and 2-methyl-6-(alpha-aminobenzyl)thiazolo[3,2-b]-1,2,4-triazole-5-ol (2a-4g) structures were synthesized. The structures of the compounds were proved by spectral and elemental analysis. All of the compounds synthesized were tested for their anti-inflammatory actively and ulcerogenic potential in mice at 10, 20 and 40 mg/kg dose levels. Compound 4b showed higher anti-inflammatory activity than the analogue derivatives and indometacin (CAS 53-86-1), used as a reference drug, at 10 mg/kg dose level. Generally, the compounds were found to be more reliable than indometacin since they did not cause any reaction in the stomach.
Tozkoparan
B
B
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Sihhiye-Ankara, Turkey.
Aktay
G
G
Yesilada
E
E
Ertan
M
M
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D002351:Carrageenan; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D013055:Spectrophotometry, Infrared; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013844:Thiazoles; D014230:Triazoles; D002351:Carrageenan