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开发对革兰阳性菌有强抗菌活性的新药是近年来喹诺酮领域的研究重点。四十多年的广泛研究,特别是近几年的研究,使人们对同时具有最佳抗革兰阳性菌活性和低耐药选择性特点的喹诺酮类的结构特征有了比较明确的认识。为了今后在设计、合成对革兰阳性菌,特别是对喹诺酮耐药的革兰阳性菌具有更满意活性的新喹诺酮时的设计策略给予启迪,本文从以下4个方面综述了新喹诺酮的结构特征及其对革兰阳性菌的构-效关系:(1)喹诺酮抗革兰阳性菌活性的演变;(2)构-效关系;(3)喹诺酮对革兰阳性菌中靶酶的取向与其结构的关系;(4)革兰阳性菌的耐药性及喹诺酮结构对其的影响。
The development of new drugs with strong antibacterial activity against Gram-positive bacteria has been the focus of research in the field of quinolones in recent years. Over forty years of extensive research, especially in recent years, have led to a clear understanding of the structural characteristics of quinolones, which have the best combination of activity against Gram-positive bacteria and low resistance to sequestration. In order to give some enlightenment in the future when designing and synthesizing new quinolones that have more active activity against Gram-positive bacteria, especially quinolone-resistant Gram-positive bacteria, this article reviews the structural features of new quinolones from the following four aspects (1) the evolution of quinolone-resistant Gram-positive bacteria activity; (2) the structure-activity relationship; (3) the orientation and structure of quinolone target enzyme in Gram-positive bacteria (4) Gram-positive bacteria resistance and quinolone structure of its impact.