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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antibacterial activity of 2-(4-substituted phenyl)-3(2H)-isothiazolones.
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Synthesis and antibacterial activity of 2-(4-substituted phenyl)-3(2H)-isothiazolones.

机译：2-（4-取代的苯基）-3（2H）-异噻唑酮的合成和抗菌活性。

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摘要

Several new and known 2-(4-substituted phenyl)-3(2H)-isothiazolone derivatives with or without chloro substituent at C-5 position were synthesized and their in vitro antibacterial activity against selected Gram-negative and Gram-positive bacteria were evaluated using agar dilution method. Most of compounds exhibited moderate to high activities against tested microorganisms, and in comparison with the reference drugs some compounds showed comparable or higher activities. In contrast to results of the previous studies, some 5-chloro derivatives showed lower or comparable activities against some tested microorganism, in comparison with analogues without C-5 substitution. In general, most of the compounds bearing electron withdrawing group at 4-position of the phenyl ring were more active against Gram-positive and most of those having piperazine derivatives were more active against Gram-negative bacteria.
机译：合成了几种新的已知的2-（4-取代的苯基）-3（2H）-异噻唑酮衍生物，在C-5位置带有或不带有氯取代基，并评估了它们对所选革兰氏阴性和革兰氏阳性细菌的体外抗菌活性用琼脂稀释法。大多数化合物对被测微生物表现出中等至高活性，与参比药物相比，某些化合物表现出可比或更高的活性。与以前的研究结果相反，与没有C-5取代的类似物相比，某些5-氯衍生物对某些被测微生物表现出较低或相当的活性。通常，大多数在苯环的4位带有吸电子基团的化合物对革兰氏阳性菌更具活性，而大多数具有哌嗪衍生物的化合物对革兰氏阴性菌则更具活性。

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