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Thioridazine: resurrection as an antimicrobial agent?

机译:硫代达嗪:作为抗菌剂复活吗?

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The emergence of multiresistant bacterial strains and the continuing burden of infectious disease globally point to the urgent need for novel affordable antimicrobial drugs. Thioridazine is a phenothiazine antipsychotic drug with well-recognized antimicrobial activity, but this property has not been harnessed for clinical use as a result of its central nervous system and cardiac side-effects. The cardiotoxicity of thioridazine has recently been shown to be structurally specific at a molecular level, whereas its antimicrobial properties are shared by a number of phenothiazine analogues. This raises the possibility that its enantiomers or its inactive metabolite, the ring sulphoxide, may act as a lead compound in the future development of antimicrobial drugs to face the new challenges in infectious disease.
机译:全球范围内多重耐药细菌菌株的出现和传染病的持续负担表明,迫切需要新型的负担得起的抗菌药物。噻哒嗪是一种吩噻嗪类抗精神病药,具有公认的抗菌活性,但由于其中枢神经系统和心脏副作用,尚未将该特性用于临床。最近已显示出硫哒嗪的心脏毒性在分子水平上具有结构特异性,而许多吩噻嗪类似物均具有抗微生物特性。这就增加了其对映异构体或其非活性代谢产物环亚砜可能在未来抗菌药物开发中担当先导化合物的角色,以应对传染病的新挑战。

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