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某些2-芳基-3-[N-(2/3/4-苯并咪唑-2-基)苯基]亚氨基亚甲基吲哚的抗结核和中枢神经系统活性

Antitubercular and CNS activities of some 2-aryl-3-[N-(2/3/4-benzimidazol-2-yl)phenyl]iminomethylenyl indoles.

作者信息

Agarwal R, Agarwal C, Kumar P

出版信息

Pharmacol Res Commun. 1984 Aug;16(8):831-44. doi: 10.1016/s0031-6989(84)80059-4.

Abstract

The title 2-aryl-3-[N-(2/3/4-benzimidazol 2yl)phenyl]iminomethylenyl indoles were synthesised by condensing 2-aryl-indol-3-aldehydes with 2-(2/3/4-aminophenyl)benzimidazoles in isopropanol and characterised by elemental and spectral (IR, PMR) studies. Compounds were screened in vivo for toxicity and gross CNS effects on albino mice and in vitro for antitubercular activity against human tuberculosis bacteria, Mycobacterium tuberculosis, H37RV. The tested compounds were nontoxic and CNS depressant. Some of them have been found to possess significant antitubercular activity, comparable with streptomycin.

摘要

标题为2-芳基-3-[N-(2/3/4-苯并咪唑-2-基)苯基]亚氨基亚甲基吲哚的化合物是通过2-芳基吲哚-3-醛与2-(2/3/4-氨基苯基)苯并咪唑在异丙醇中缩合反应合成的,并通过元素分析和光谱(红外光谱、核磁共振氢谱)研究进行了表征。对这些化合物进行了体内毒性和对白化病小鼠中枢神经系统总体影响的筛选,以及体外对人结核分枝杆菌H37RV的抗结核活性筛选。测试的化合物无毒且具有中枢神经系统抑制作用。其中一些化合物已被发现具有显著的抗结核活性,与链霉素相当。

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