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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antimicrobial properties of 2-(benzylidene-amino)-benzo(d)isothiazol-3-ones.
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Synthesis and antimicrobial properties of 2-(benzylidene-amino)-benzo(d)isothiazol-3-ones.

机译：2-（亚苄基-氨基）-苯并（d）异噻唑-3-酮的合成及抗菌性能。

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摘要

The in vitro antimicrobial activity of 2-amino-benzo[d]isothiazol-3-one and of several 2-arylideneamino derivatives carrying in the second position a substituted or unsubstituted aromatic ring or an arylalkenylidene moiety was determined by the broth dilution method against several strains selected to define their spectrum and potency. All the compounds demonstrated good antibacterial properties against Bacillus subtilis, streptococci, enterococci and staphylococci including penicillin-resistant clinical isolates. Several compounds showed excellent inhibitory properties against Streptococcus pyogenes, which is the most sensitive microorganism tested. Many benzisothiazolones exhibited good activity against Gram-negative Haemophilus influenzae. As regards antifungal activity, several of the tested compounds inhibited Saccharomyces cerevisiae at concentrations of 3-6 microg ml-1. In all cases the parent 2-amino-benzo[d]isothiazol-3-one was the most effective agent, with minimum inhibitory concentration (MIC) values ranging from 0.07 to 6 microg ml-1. The results obtained indicate that most of these compounds are wide-spectrum antimicrobial substances and promising agents against penicillin-resistant staphylococci.
机译：通过肉汤稀释法测定2-氨基-苯并[d]异噻唑-3-酮和几种在第二位置带有取代或未取代的芳环或芳基亚烯基部分的2-亚芳基氨基衍生物的体外抗菌活性。选择用于定义其光谱和效能的菌株。所有化合物对枯草芽孢杆菌，链球菌，肠球菌和葡萄球菌均具有良好的抗菌性能，包括耐青霉素的临床分离株。几种化合物对化脓性链球菌具有极好的抑制特性，而化脓性链球菌是经测试的最敏感的微生物。许多苯并异噻唑酮对革兰阴性流感嗜血杆菌表现出良好的活性。关于抗真菌活性，一些测试的化合物在3-6微克ml-1的浓度下抑制了酿酒酵母。在所有情况下，母体2-氨基-苯并[d]异噻唑-3-酮是最有效的药物，最小抑菌浓度（MIC）值范围为0.07至6 microg ml-1。获得的结果表明，这些化合物大多数是广谱抗菌物质，并且是抗青霉素耐药葡萄球菌的有前途的药物。

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