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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and pharmacological properties of some 4-arylhydrazono-2-pyrazoline-5-one derivatives obtained from heterocyclic amines.
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Synthesis, characterization and pharmacological properties of some 4-arylhydrazono-2-pyrazoline-5-one derivatives obtained from heterocyclic amines.

机译：从杂环胺获得的一些4-芳基肼基-2-吡唑啉-5-一衍生物的合成，表征和药理特性。

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摘要

The synthesis of a new series of 4-arylhydrazono-2-pyrazoline-5-ones 7-24 and 22a is described. Structures of the synthesized compounds were confirmed using UV, IR, 1H-NMR, 13C-NMR and EI-mass spectral data. These compounds were tested in vitro against one Gram-positive and two Gram-negative bacterial strains, two mycobacterial strains and a fungus, Candida albicans. Compound 22 was found to be more active against Staphylococcus aureus than the other compounds at a concentration of 15.6 microg/mL. Some related compounds were evaluated for anticonvulsant activity. Compound 11 showed 40% protection against pentylenetetrazole-induced seizures in albino Swiss mice. In vitro antituberculosis activity of 4-arylhydrazono-2-pyrazoline-5-ones 7-12, 14-24, 22a and coupling products 6a-f were tested on Mycobacterium tuberculosis H37Rv. Of these compounds, only 24, which exhibited > 90% inhibition in the primary screen at 12.5 microg/mL against this strain was re-examined for determination of its actual MIC. However, level II assay revealed that the MIC value was not less than 12.5 microg/mL. The same compound was also tested against Mycobacterium avium, which was observed not to be susceptible to 24.
机译：描述了新系列的4-芳基肼基-2-吡唑啉-5-酮7-24和22a的合成。使用UV，IR，1 H-NMR，13 C-NMR和EI-质谱数据确认合成的化合物的结构。这些化合物在体外针对一种革兰氏阳性和两种革兰氏阴性细菌菌株，两种分枝杆菌菌株和一种真菌白色念珠菌进行了测试。发现化合物22对金黄色葡萄球菌的活性比其他化合物高，浓度为15.6 microg / mL。评价一些相关化合物的抗惊厥活性。化合物11在白化病瑞士小鼠中显示出40％的抗戊四唑诱导的癫痫发作的保护作用。在结核分枝杆菌H37Rv上测试了4-芳基肼基-2-吡唑啉-5-酮7-12、14-24、22a和偶联产物6a-f的体外抗结核活性。在这些化合物中，只有24种在初筛中以12.5 microg / mL的抗性表现出> 90％的抑制作用，需要重新检查以确定其实际MIC。但是，II级分析显示MIC值不小于12.5 microg / mL。还测试了相同的化合物抗鸟分枝杆菌，观察到它对24不敏感。

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