6-benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted with ibuprofen:: synthesis, characterization and evaluation of anti-inflammatory activity

被引:188
作者
Tozkoparan, B
Gökhan, N
Aktay, G
Yesilada, E
Ertan, M
机构
[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey
[2] Ankara Univ, Inst Forens Med, Toxicol Unit, TR-06100 Ankara, Turkey
[3] Gazi Univ, Fac Pharm, Dept Pharmacognosy, Ankara, Turkey
关键词
3-[1-(4-(2-methylpropyl)phenyl)ethyl]-1,2,4-triazole-5-thione; 6-benzylidenethiazalo[3,2-b]-1,2,4-triazole-5(6H)-ones; synthesis; anti-inflammatory activity;
D O I
10.1016/S0223-5234(00)00157-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In this study, the synthesis of 3-[1-(4-(2-methylpropyl)phenyl)ethyl]-1,2,4-triazole-5-thione (2) and its condensed derivatives 6-benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (2a-u) are described. The structures of the compounds were elucidated by spectral and elemental analysis. In the pharmacological studies, anti-inflammatory activities of these compounds have been screened. Among the compounds examined, the compounds 2 and 2g possessed the most prominent and consistent activity. In gastric ulceration studies the synthesized compounds were generally found to be safe at a 200 mg/kg dose level. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
引用
收藏
页码:743 / 750
页数:8
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