氟喹诺酮类杂合体的抗耐药菌活性

The anti-drug-resistant bacteria activity of fluoroquinolone hybrids

抗生素是治疗细菌感染的主要手段。然而,由于长时间对其不恰当使用甚至滥用,耐药菌不断涌现,导致传统抗生素的疗效不断下降。目前,治疗耐药菌感染的疗法屈指可数。因此,耐药菌已严重威胁人类生命健康,开发新型抗耐药菌药物势在必行。喹诺酮尤其是氟喹诺酮类抗生素是仅次于头孢菌素类药物的第二大类抗生素,具有抗菌谱广、抗菌活性高和毒副作用低等特点,在临床上广泛用于各种细菌感染的治疗。尽管致病菌对喹诺酮类抗生素也产生了耐药性,喹诺酮杂合体由于嵌入了其他抗菌药效团,可同时作用于不同的药物靶点,具有克服耐药性的潜力。本文将着重介绍近5年来所开发的具有抗耐药菌活性的喹诺酮杂合体的最新研究进展,为进一步合理设计此类杂合体提供一定的理论支持。

Antibiotics are the mainstay for the treatment of bacterial infections.The rapid development of drug-resistant bacteria due to the improper and overuse of antibiotics has been severely affected clinical effectiveness of current available conventional antibiotics.Due to the limitation of effective drugs,drug-resistant bacteria have already become one of the daunting global challenges,calling for novel antibiotics with anti-drug-resistant bacterial potential.Fluoroquinolones possess broad antibacterial spectrum,high activity,and low side effects.Accordingly,fluoroquinolone antibiotics are widely used in clinical treatment of various bacterial infections.Although pathogens have also developed resistance to fluoroquinolone antibiotics,fluoroquinolone hybrids embedding other antibacterial pharmacophores can act on different drug targets at the same time and have the potential to overcome drug resistance.This manuscript discusses the anti-drug-resistant bacteria activity of fluoroquinolone hybrids and summarizes the structure-activity relationship.