喹诺酮类药物的抗菌活性与细菌耐药性研究进展

doi:10.16431/j.cnki.1671-7236.2017.09.033

Abstract

Abstract:

Quinolones (QLs) are synthetic antimicrobials and widely used to treat clinical bacterial disease in the world. Quinolones trap DNA gyrase or topoisomerase Ⅳ to form reversible drug-enzyme-DNA complexes and prevent protein synthesis,resulting in bacteriostasis. Recently, the analysis of crystal structures of cleaved complexes and building of the model of noncatalytic magnesium ion present a reasonable explanation for the phenomenon of the effect of quinolones antibacterial activity. There are many researches for the mechanisms of resistance of quinolones, gene mutation, altered drug permeation and plasmid-mediated quinolone resistance are three main aspects. Here, the molecular basis for the antibacterial action and mechanisms of resistance of quinolones were fully discussed and updated, so as to provide a large number of information for optimization of quinolone antimicrobials based on structural transformation.

Key words: quinolones; mechanism; drug-resistant mechanism

CLC Number:

SHAO Li-ping, ZHANG Ji-yu. Research Advances on Antibacterial Activity and Bacterial Resistance of Quinolones[J]. , 2017, 44(9): 2773-2782.

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Research Advances on Antibacterial Activity and Bacterial Resistance of Quinolones

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