Synthesis and Antimicrobial Evaluation of Some Novel 2-(Hydroxyimino)-dihydropyrimidine-5-carboxylic acids

R. Shastri, Post
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Abstract

: A series of of 1,2,3,4-tetrahydro-2-(hydroxyimino)-6-methyl/1,6-dimethyl-4-phenyl pyrimidine-5-carboxylic acid (2a-o) were prepared by refluxing ethyl-1,2,3,4-tetrahydro-6-methyl/1,6-dimethyl-2-oxo-4-phenylpyrimidine-5-carboxylate (1a-o) with hydroxylamine hydrochloride in the presence of sodium hydroxide, yielded (2a-o) in excellent yields. The advantages of this method is excellent yields, short reaction time, no side reaction and operational simplicity and ease product isolation The structure of all the synthesized compounds were characterized by FT-IR, 1 H NMR and MS data. The compounds 2a-o has been screened for their antimicrobial activity. All the compounds possesses significant to moderate antibacterial activity and promising antifungal activity.
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新型2-(羟亚胺)-二氢嘧啶-5-羧酸的合成及抗菌性能评价
在氢氧化钠存在下,用盐酸羟胺与乙基-1,2,3,4-四氢-6-甲基/1,6-二甲基-2-氧-4-苯基嘧啶-5-羧酸(1a-o)回流制得一系列1,2,3,4-四氢-2-(羟亚胺)-6-甲基/1,6-二甲基-4-苯基嘧啶-5-羧酸(1a-o),产率高。该方法具有收率高、反应时间短、无副反应、操作简单、易于分离等优点。所有合成化合物的结构均通过FT-IR、1h NMR和MS数据进行了表征。对化合物2a-o的抑菌活性进行了筛选。所有化合物均具有显著至中等抑菌活性,具有良好的抗真菌活性。
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