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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents.
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Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents.

机译：某些4-官能化吡唑类抗菌剂的合成及生物学评价。

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摘要

1,3-Diaryl-4-formylpyrazoles 8 bearing benzenesulfonamide moiety at position-1 were synthesized as important intermediates following Vilsmeier-Haack strategy. Aldehyde moiety of 4-formylpyrazole was then converted into carboxylic acid 9, cyano 10 and carbothioamide 11 using established procedures. Out of these 4-functionalized pyrazoles, pyrazole-4-carboxylic acids 9 and carbothioamides 11 were evaluated for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative), and in vitro antifungal activity against two pathogenic fungal strains namely, Aspergillus niger and Aspergillus flavus. Three tested compounds, 9e, 11b and 11f exhibited moderate antibacterial activity against Gram-positive bacteria and 9g showed moderate antifungal activity against the tested fungi. However, none of the compounds showed any activity against Gram-negative bacteria.
机译：根据Vilsmeier-Haack策略，合成了在位置1处带有苯磺酰胺部分的1，3-二芳基-4-甲酰基吡唑8作为重要的中间体。然后使用确定的方法将4-甲酰基吡唑的醛部分转化为羧酸9，氰基10和碳硫酰胺11。在这4种官能化的吡唑中，对4种致病细菌菌株，即金黄色葡萄球菌，枯草芽孢杆菌（革兰氏阳性），大肠杆菌，铜绿假单胞菌（革兰氏阴性）和体外对两种病原性真菌菌株黑曲霉和黄曲霉的抗真菌活性。三种被测化合物9e，11b和11f对革兰氏阳性菌表现出中等的抗菌活性，而9g对被测真菌表现出中等的抗真菌活性。但是，没有一种化合物对革兰氏阴性菌显示任何活性。

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