非喹诺酮类细菌ⅡA型拓扑异构酶抑制剂的研究进展  

Advances in research of non-quinolone bacterial type ⅡA topoisomerase inhibitors

作　　者：马洁 李荀 刘兆鹏[1] MA Jie;LI Xun;LIU Zhao-peng(School of Pharmaceutical Sciences,Shandong University,Jinan 250012,China;Institute of Materia Medica,Shandong First Medical University,Jinan 250002,China)

机构地区：[1]山东大学药学院,山东济南250012 [2]山东第一医科大学药物研究所,山东济南250002

出　　处：《中国药物化学杂志》2021年第11期911-920,共10页Chinese Journal of Medicinal Chemistry

摘　　要：细菌ⅡA型拓扑异构酶(DNA促旋酶和拓扑异构酶Ⅳ)是控制细菌感染的有效靶标。喹诺酮类抗生素是目前临床上广泛应用的细菌ⅡA型拓扑异构酶抑制剂,由于不合理使用以及滥用,导致细菌ⅡA型拓扑异构酶与喹诺酮类药物的结合位点发生突变,使细菌对其产生耐药性。非喹诺酮类ⅡA型拓扑异构酶抑制剂与细菌ⅡA型拓扑异构酶的结合位点不同于喹诺酮类药物,从而对喹诺酮类耐药的细菌发挥药效。本文根据不同的化学结构类型,总结了近6年来非喹诺酮类细菌ⅡA型拓扑异构酶抑制剂的研究进展。Bacterial type ⅡA topoisomerases(DNA gyrase and topoisomerase Ⅳ) are valid targets to control infection.Quinolones act via inhibiting type ⅡA topoisomerase and they are currently the most widely used drugs in clinical practice.However, due to unreasonable use or even abuse of quinolone, the quinolone binding site of bacterial type ⅡA topoisomerases has mutated, which makes the bacteria develop drug resistance.The binding site of non-quinolone type ⅡA topoisomerase inhibitors with type ⅡA topoisomerase are different from that of quinolone drugs, and can be effective against quinolone-resistant bacteria.This article summarized the research progress of different structural types of non-quinolone type ⅡA topoisomerase inhibitors in the past six years.

关 键 词：细菌ⅡA型拓扑异构酶抑制剂 ⅡA型拓扑异构酶 抗菌 

分 类 号：R914[医药卫生—药物化学]