喹诺酮类药物构效关系及结构改造的研究进展

Advances in the Study of Transformation on the Structure of Quinolones and Its Structure-Activity Relationships

在喹诺酮类药物基本结构的基础上 ,综述了从萘啶酸开始 ,第一代至第四代药物结构改造的过程 .当用不同的基团取代喹诺酮类环上的不同位置时发现 ,这直接影响到此类药物的抗菌活性及药代动力学性质 ,且环上的C -1、C - 6及C - 7位是喹诺酮类药物结构中重要的活性部位 .

The paper reviews the recent advances in studies on the transformation of Quinolones based on its basic structure. The review includes all the four generations of Quinolones,beginning from Nalidixic acid.And we put different structure on different positions and have disclosed the relationships between Quinolones’ chemical structure and its antibacterial activity、pharmacokinetics properties.We have also found that the C-1、C-6 and C-7 are important positions in the structure of Quinolones.