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设计、合成及一些新型噻吩并嘧啶和稠合噻吩并嘧啶类化合物的抗炎活性评价。

Design, synthesis and biological evaluation of some novel thienopyrimidines and fused thienopyrimidines as anti-inflammatory agents.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, 1 Meedan Elkhartoom, Alexandria 21521, Egypt.

出版信息

Eur J Med Chem. 2012 Sep;55:85-93. doi: 10.1016/j.ejmech.2012.07.007. Epub 2012 Jul 14.

DOI:10.1016/j.ejmech.2012.07.007
PMID:22835720
Abstract

Some new substituted thienopyrimidine derivatives comprising thioxo, thioalkyl and pyrazolyl derivatives as well as fused thienotriazolopyrimidine and thienopyrimidinotriazine ring systems were prepared from 3-benzyl-2-hydrazino-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide 4. The designed compounds were evaluated for their anti-inflammatory activity. Compounds 4, 9, 10 and 13 showed the highest anti-inflammatory effect compared with the reference drug diclofenac sodium.

摘要

一些新的取代噻吩并嘧啶衍生物,包括噻噁、硫代烷基和吡唑基衍生物,以及稠合的噻吩并三唑并嘧啶和噻吩并嘧啶并三嗪环系统,是由 3-苄基-2-肼基-5-甲基-4-氧代-3,4-二氢噻吩并[2,3-d]嘧啶-6-甲酰胺 4 制备的。设计的化合物被评估了其抗炎活性。与参考药物双氯芬酸钠相比,化合物 4、9、10 和 13 表现出最高的抗炎效果。

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