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J Enzyme Inhib Med Chem:新型抗菌剂可有效抗菌

2018-05-04 MedSci MedSci原创

多药耐药性细菌感染的发病率逐渐增加,迫切需要开发新的抗生素。开发干扰FtsZ活性的小分子是一种有前途的用于寻求高效力抗菌药物的方法。本研究中,研究人员合成了一系列新的喹啉衍生物并探究其抗菌活性。结果显示,这些化合物对包括MRSA,VRE和NDM-1大肠杆菌在内的不同细菌菌株具有很强的抗菌活性。在这些衍生物中,含有4-氟苯基(A2)的化合物表现出优异的抗菌活性,其对耐药菌株的MICs低于甲氧西林和万

多药耐药性细菌感染的发病率逐渐增加,迫切需要开发新的抗生素。开发干扰FtsZ活性的小分子是一种有前途的用于寻求高效力抗菌药物的方法。本研究中,研究人员合成了一系列新的喹啉衍生物并探究其抗菌活性。

结果显示,这些化合物对包括MRSA,VRE和NDM-1大肠杆菌在内的不同细菌菌株具有很强的抗菌活性。在这些衍生物中,含有4-氟苯基(A2)的化合物表现出优异的抗菌活性,其对耐药菌株的MICs低于甲氧西林和万古霉素。生物学结果表明,这些喹啉衍生物可以破坏GTP酶活性和FtsZ的动态组装,从而抑制细菌细胞分裂,然后导致细菌死亡。

综上所述,该研究结果表明,这些化合物值得进一步评估开发针对FtsZ的新型抗菌剂。

原始出处:


Sun N, Du RL, et al., Antibacterial activity of 3-methylbenzo[d]thiazol-methylquinolinium derivatives and study of their action mechanism. J Enzyme Inhib Med Chem. 2018 Dec;33(1):879-889. doi: 10.1080/14756366.2018.1465055.

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    2018-05-04 1e0f8808m18(暂无匿称)

    新型抗菌剂.抗细菌利器.

    0

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    2018-05-04 清风拂面

    谢谢分享学习

    0

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    2018-05-04 天地飞扬

    了解一下.谢谢分享!

    0

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