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Synthesis and antimicrobial activities of new 4-thiazolidones derived from formipyridine thiosemicarbazones

机译:甲酰吡啶硫代半氨基咔唑新的4-噻唑烷酮类化合物的合成及抑菌活性

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摘要

Twelve novel 4-thiazolidinone derivatives (2a-l) have been synthesized by reacting formilpyridine thiosemicarbazones (1a-l) and anhydride maleic in toluene. Their chemical structures were confirmed by IR, 1H and 13C NMR. The new compounds were submitted to in vitro evaluation against pathogenic Gram-positive, Gram-negative bacteria and yeasts. The findings obtained showed that the compounds 2a, 2d, 2e and 2g were effective against some of the bacterial strains used, whereas the compounds 2d, 2e and 2i exhibited a moderate antifungal activity against the yeast strains evaluated. An initial structure activity relationship (SAR) was established.
机译:通过使甲吡啶吡啶硫代半咔唑酮(1a-1)与马来酸酐酐在甲苯中反应,已经合成了十二种新颖的4-噻唑烷酮衍生物(2a-1)。它们的化学结构通过IR,1 H和13 C NMR证实。这些新化合物已提交给针对致病性革兰氏阳性,革兰氏阴性细菌和酵母菌的体外评估。获得的发现表明,化合物2a,2d,2e和2g对所用的某些细菌菌株有效,而化合物2d,2e和2i对所评价的酵母菌株表现出中等的抗真菌活性。建立了初始结构活动关系(SAR)。

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