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用布洛芬取代的6-亚苄基噻唑并[3,2-b]-1,2,4-三唑-5(6H)-酮:合成、表征及抗炎活性评价

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

作者信息

Tozkoparan B, Gökhan N, Aktay G, Yeşilada E, Ertan M

机构信息

Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 06100 Sihhiye, Ankara, Turkey.

出版信息

Eur J Med Chem. 2000 Jul-Aug;35(7-8):743-50. doi: 10.1016/s0223-5234(00)00157-4.

Abstract

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.

摘要

本研究描述了3-[1-(4-(2-甲基丙基)苯基)乙基]-1,2,4-三唑-5-硫酮(2)及其缩合衍生物6-亚苄基噻唑并[3,2-b]-1,2,4-三唑-5(6H)-酮(2a-u)的合成。通过光谱和元素分析阐明了这些化合物的结构。在药理学研究中,对这些化合物的抗炎活性进行了筛选。在所研究的化合物中,化合物2和2g具有最显著且一致的活性。在胃溃疡研究中,通常发现合成化合物在200mg/kg剂量水平下是安全的。

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