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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, structural activity relationship and anti-tubercular activity of novel pyrazoline derivatives.
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Synthesis, structural activity relationship and anti-tubercular activity of novel pyrazoline derivatives.

机译：新型吡唑啉衍生物的合成，结构活性关系和抗结核活性。

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摘要

In the present investigation, a series of 5-(-4-(substituted) phenyl)-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolyl-2-toluidin o methane thione and 5-(substituted) phenyl-3-(4-hydroxy-3-methylphenyl)-4,5-dihydro-1H-1-pyrazolyl-2-methoxyan ilino methane thione were synthesized by the reaction between hydrazine hydrate and chalcones (3a-k) followed by condensation with appropriate aryl isothiocyanate which yielded N-substituted pyrazoline derivatives. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. Among the synthesized compounds, compound anilino-3-(4-hydroxy-3-methylphenyl)-5-(2,6-dichlorophenyl)-4,5-dihydro-1H -1-pyrazolylmethanethione (6i) was found to be more active agent against M. tuberculosis H37Rv with minimum inhibitory concentration of 0.0034 microM.
机译：在本研究中，一系列的5-（-4-（取代）苯基）-3-（4-羟基-3-甲基苯基）-4,5-二氢-1H-1-吡唑基-2-甲苯胺或甲烷硫酮通过水合肼与查耳酮的反应合成5-（取代的）苯基-3-（4-羟基-3-甲基苯基）-4,5-二氢-1H-1-吡唑基-2-甲氧基茚满甲烷硫酮（3a -k），然后与适当的异硫氰酸芳基酯缩合，得到N-取代的吡唑啉衍生物。使用BACTEC 460辐射系统测试了新合成的化合物对结核分枝杆菌H37Rv的体外抗结核活性。在合成的化合物中，发现化合物苯胺基-3-（4-羟基-3-甲基苯基）-5-（2,6-二氯苯基）-4,5-二氢-1H -1-吡唑基甲烷硫酮（6i）更具活性抗结核分枝杆菌H37Rv的药物，最低抑制浓度为0.0034 microM。

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