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合成及部分 6-芳基-5-氰基-2-硫代尿嘧啶衍生物的抗菌活性评价。

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivatives.

机构信息

Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt.

出版信息

Acta Pharm. 2011 Jun;61(2):171-85. doi: 10.2478/v10007-011-0019-1.

Abstract

A series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-d to 10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2d), 6-(4-fluorophenyl)-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-cabonitrile (7a) and 4-hydrazino-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrimidine-5-carbonitrile (7d) revealed promising antimicrobial activity.

摘要

通过乙腈酸乙酯与硫脲和醛的反应,合成了一系列 6-芳基-5-氰基-2-硫代尿嘧啶衍生物(1a-d)。这些产物被用作合成一系列硫代尿嘧啶衍生物(2a-d 至 10a-d)的中间化合物。所有化合物都进行了抗菌和抗真菌活性筛选。一些制备的化合物,如 6-(4-氟苯基)-4-氧代-2-硫代-1,2,3,4-四氢嘧啶-5-甲酰胺(2a)、4-氧代-2-硫代-6-(3,4,5-三甲氧基苯基)-1,2,3,4-四氢嘧啶-5-甲酰胺(2d)、6-(4-氟苯基)-4-肼基-2-硫代-1,2-二氢嘧啶-5-甲腈(7a)和 4-肼基-2-硫代-6-(3,4,5-三甲氧基苯基)-1,2-二氢嘧啶-5-甲腈(7d),显示出有希望的抗菌活性。

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