微波辅助合成几种2-氨基-6-芳基-4-(2-噻吩基)嘧啶及其抗菌活性

S. Chandrasekaran, S. Nagarajan
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引用次数: 37

摘要

以3-芳基-1-硫基-2-烯-1-酮和盐酸胍为原料,在碱存在下,通过酒精介质常规加热和无溶剂条件下微波加热,合成了几种新型的2-氨基-6-芳基-4-(2-噻吩基)嘧啶。对化合物进行体外抑菌活性评价。结果表明,化合物5a-e对革兰氏阳性菌的抑菌活性优于对照物环丙沙星和诺氟沙星。然而,这些化合物对革兰氏阴性菌几乎没有活性。化合物5c和e对革兰氏阳性菌的抑菌活性最强。
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Microwave-assisted synthesis and anti-bacterial activity of some 2-Amino-6-aryl-4-(2-thienyl)pyrimidines

Some novel 2-amino-6-aryl-4-(2-thienyl)pyrimidines were synthesized from 3-aryl-1-thien-2ylprop-2-en-1-ones and guanidine hydrochloride in presence of alkali by conventional heating in alcoholic medium and microwave heating in solvent-free conditions. The compounds were evaluated for in vitro anti-bacterial activity. The anti-bacterial data revealed that compounds 5ae had better activity against tested Gram-positive organisms than the reference ciprofloxacin and norfloxacin. However, the compounds were nearly inactive against Gram-negative bacteria. Compounds 5c and e were the most active compounds against Gram-positive bacteria.

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