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Synthesis and antimicrobial evaluation of some 4- or 6-chloroisatin derivatives

机译:某些4-或6-氯异丁香素衍生物的合成和抗菌评估

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Two series of chloroisatin-3-semicarbazones and hydrazones have been designed and prepared by condensing 4-chloro and 6-chloroisatin with several substituted semicarbazides and related bioisosteric hydrazides,respectively.Investigation of in vitro antimicrobial activity of compounds has been performed by agar double dilution method against nine pathogenic bacteria and four pathogenic fungi.The title compounds are also screened for their antilubcrcular activity against Mycobacterium tuberculosis H_(37) R_v using microplate alamar blue assay.Many of the synthesized compounds exhibit significant antibacterial activity in comparison to sulphamcthoxazole,trimethoprim and some compounds show good antifungal activity comparable to clotrimazole.The semicarbazones arised from the 6-chloroisatin series have exhibited good antimicrobial activity than that obtained from 4-chloroisatins.Compounds,6-chloroisatin-3-(2'-chlorophenyl) semicarbazones 1b and 6-chloroisatin-3-(4'-bromophenyl) semicarbazone 4b have shown a promising activity in both antibacterial and antifungal screenings.None of the compounds has been found to be active in antilubcrcular screening.
机译:通过将4-氯和6-氯异丁香素分别与几种取代的氨基脲和相关的生物甾体酰肼缩合,设计和制备了两个系列的氯异丁香3-半咔唑酮和。通过琼脂两次稀释进行化合物的体外抗菌活性研究对9种病原菌和4种病原真菌的分离方法。使用微量培养板alamar蓝法还筛选了标题化合物对结核分枝杆菌H_(37)R_v的抗润滑活性。一些化合物具有与克霉唑相当的抗真菌活性。6-氯异丁香系列衍生的半咔唑酮比4-氯异丁香酮具有更好的抗菌活性。化合物6-氯异丁香-3-(2'-氯苯基)半咔唑酮1b和6 -chloroisatin-3-(4'-溴苯基)氨基脲e 4b在抗菌和抗真菌筛选中均显示出有希望的活性。未发现这些化合物在抗润滑性筛选中具有活性。

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