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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Novel 4-(morpholin-4-yl)-N'-(arylidene)benzohydrazides: synthesis, antimycobacterial activity and QSAR investigations.
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Novel 4-(morpholin-4-yl)-N'-(arylidene)benzohydrazides: synthesis, antimycobacterial activity and QSAR investigations.

机译：新型的4-（吗啉-4-基）-N'-（亚芳基）苯并酰肼：合成，抗分枝杆菌活性和QSAR研究。

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摘要

A series of 4-(morpholin-4-yl)-N'-(arylidene)benzohydrazides were synthesized using appropriate synthetic route. Antimycobacterial activity of the synthesized compounds (5a-5j) was carried out and percentage reduction in relative light units (RLU) was calculated using luciferase reporter phages (LRP) assay. Percentage reduction in relative light units (RLU) for isoniazid was also calculated. The test compounds showed significant antitubercular activity against Mycobacterium tuberculosis H37Rv and clinical isolates: S, H, R, and E resistant M. tuberculosis, when tested in vitro. Quantitative structure-activity relationship (QSAR) investigation with 2D-QSAR analysis was applied to find a correlation between different experimental or calculated physicochemical parameters of the compounds studied and 3D-QSAR analysis and to indicate the exact steric and electronic requirements in the ranges at various positions around pharmacophore. In general Schiff bases exhibit antimycobacterial activity and morpholine ring is important for antimicrobial activity. So we have synthesized 10 different 4-(morpholin-4-yl)-N'-(arylidene)benzohydrazides. The structures of new compounds were characterized by TLC, FTIR, (1)H NMR, mass spectral data and elemental analysis. Amongst the compounds tested 5d and 5c were found to be the most potent, while 5i, 5e, and 5j were found to have an average activity against M. tuberculosis H37Rv and 5a, 5f, 5h, 5g, and 5b were found to have a greater activity against clinical isolates: S, H, R, and E resistant M. tuberculosis as compared to M. tuberculosis H37Rv.
机译：使用适当的合成途径合成了一系列的4-（吗啉-4-基）-N'-（亚芳基）苯并酰肼。进行了合成化合物（5a-5j）的抗分枝杆菌活性，并使用萤光素酶报告基因噬菌体（LRP）测定了相对光单位（RLU）的降低百分比。还计算了异烟肼的相对光单位（RLU）减少的百分比。当在体外进行测试时，测试化合物对结核分枝杆菌H37Rv和临床分离株：S，H，R和E耐药结核分枝杆菌显示出显着的抗结核活性。应用2D-QSAR分析进行定量构效关系（QSAR）研究，以发现所研究化合物的不同实验或计算的理化参数之间的相关性，并指出3D-QSAR分析的确切空间和电子要求药效团周围的位置。通常，席夫碱具有抗分枝杆菌活性，吗啉环对于抗菌活性很重要。因此，我们合成了10种不同的4-（吗啉-4-基）-N'-（亚芳基）苯并酰肼。通过TLC，FTIR，（1）H NMR，质谱数据和元素分析对新化合物的结构进行了表征。在测试的化合物中，发现5d和5c最有效，而发现5i，5e和5j具有抗结核分枝杆菌H37Rv的平均活性，发现5a，5f，5h，5g和5b具有抗结核作用。与结核分枝杆菌H37Rv相比，对临床分离株：S，H，R和E耐药的结核分枝杆菌具有更高的活性。

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