分子杂交策略设计的喹诺酮类抗菌化合物进展  

Progress in the design of quinolone antibacterial compounds based on molecular hybridization strategy

作　　者：宋润喆 郑刚[1] SONG Runzhe;ZHENG Gang(Sinopec(Beijing)Research Institute of Chemical Industry Co.,Ltd.,Beijing 100013,China)

机构地区：[1]中石化(北京)化工研究院有限公司,北京100013

出　　处：《石油化工》2024年第12期1827-1835,共9页Petrochemical Technology

摘　　要：喹诺酮类化合物是一类广泛用于细菌感染临床治疗的药物,部分药物是特定感染的首选治疗药物。随着抗菌药物的长期使用,具有新型结构的化学合成抗菌药物的研究与开发很有必要。采用分子杂交策略将两种生物活性片段糅合,可得到对靶标活性更高或作用多个靶标的新化合物,提高体内药物对疾病的整体活性,实现“1+1>2”的效果。综述了喹诺酮类抗菌药的作用机制和构效关系,概述了分子杂交策略下得到的新型喹诺酮类抗菌化合物的进展以及对喹诺酮类化合物进行优化的研究进展。Quinolone compounds are widely used in the clinical treatment of bacterial infections,and some quinolone derivatives are the first choice for treating specific infections.With the long-term use of antibacterial agents,it is necessary to develop antibacterial agents with new structures.The molecular hybridization strategy was adopted to combine two bioactive fragments to obtain new compounds with higher target activities or multiple targets to improve the overall activities of agents in vivo to the disease and achieve better effects.This paper reviewed the mechanism of action and structure-activity relationship of quinolones,the progress in novel quinolone antibacterial compounds obtained by the molecular hybridization strategy,and the research progress in the optimization of quinolone antibacterial compounds.

关 键 词：喹诺酮类 抗菌 分子杂交 

分 类 号：TQ465.91[化学工程—制药化工]