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[N-杂芳基-3(5)-硝基吡啶的合成与药理活性]

[Synthesis and Pharmacological Activity of N-Hetaryl-3(5)-Nitropyridines].

作者信息

Klimenko A I, Divaeva L N, Zubenko A A, Morkovnik A S, Fetisov L N, Bodryakov A N

出版信息

Bioorg Khim. 2015 Jul-Aug;41(4):454-61. doi: 10.1134/s1068162015030048.

Abstract

Reacting a number chlorosubstituted 3(5)-nitropyridine with some diazoles or 3-chloropyridazin-6-one synthesized previously undescribed various 2-, 4- or 6-substituted hetaryl-3(5)-nitropyridines. Furthermore, pyrazolyl-3-nitropyridine prepared by cyclizing hydrazinopyridine resulting from the nucleophilic substitution of chlorine in chlorosubstituted 3-nitropyridine by hydrazine. It has been shown that these compounds have moderate antibacterial activity against some pathogenic Gram-positive and Gram-negative bacteria (Staphylococcus aureus, Escherichia coli), as well as a strong effect on protistocidal action form Colpoda steinii, surpassing clinically used reference drugs.

摘要

使一定数量的氯代3(5)-硝基吡啶与一些二唑或先前合成的3-氯哒嗪-6-酮反应,得到了各种未描述过的2-、4-或6-取代的杂芳基-3(5)-硝基吡啶。此外,通过使氯代3-硝基吡啶中的氯被肼亲核取代而产生的肼基吡啶环化制备了吡唑基-3-硝基吡啶。已经表明,这些化合物对一些致病性革兰氏阳性和革兰氏阴性细菌(金黄色葡萄球菌、大肠杆菌)具有中等抗菌活性,并且对斯坦尼科尔波虫具有强烈的杀原生动物作用,超过了临床使用的参考药物。

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