摘要
随着耐药菌的不断出现和在世界范围内的广泛传播,感染性疾病的发病率和死亡率呈逐年上升之势。因此,研发新的抗菌药刻不容缓。氟喹诺酮是继头孢菌素之后在临床上应用最为广泛的广谱、高效、低毒性化疗药物,除经典的抗菌活性外,氟喹诺酮还具有多种"非经典"生物活性。近年来的研究表明,向药物分子中引入金属离子可对药物的生物活性产生深刻影响。因此,金属螯合药物已成为新药研发的热点方向。药物化学家对氟喹诺酮金属螯合物进行了广泛的研究,发现了若干具有潜在抗菌活性的化合物。本文归纳了近年来氟喹诺酮金属螯合物在抗菌领域的最新研究进展,为研究人员寻找新型氟喹诺酮类抗菌药提供理论依据。
The emergency and wide spread of drug-resistant bacteria represent a significant health threat throughout the world. To overcome the resistance, new antibacterials were urgently needed. Fluoroquinolones were the second widest used chemotherapy antibiotics against various bacterial infections, and they have been proven that intercalation of metals into drugs can have a profound effect on their biological activities, so fluoroquinolone-metal complexes have caused great interests in recent years. This review aims to outline the recent advances made towards the discovery of fluoroquinolone-metal complexes as potential antibacterial agents and as well as the structure-activity relationship of these derivatives. The enriched SAR paves the way for the further rational development of novel fluoroquinolones with a unique mechanism of action different from that of the currently used drugs to overcome the resistance.
作者
范一雷
刘敏
柯星
徐志
Fan Yi-Lei;Liu Min;Ke Xing;Xu Zhi(Key Laboratory of Drug Prevention and Control Technology of Zhejiang Province, Zhejiang Police College, Hangzhou 310053;College of Pharmaceutical Science ＆ Green Pharmaceutical Collaborative Innovation Center of Yangtze river Delta Region, Zhejiang University of Technology, Hangzhou 310014;Huanghuai University, Zhumadian 463000)
出处
《国外医药（抗生素分册）》
CAS
2018年第3期194-200,共7页
World Notes on Antibiotics
关键词
氟喹诺酮
金属螯合物
抗菌
构-效关系
fluoroquinolones
metal complexes
antibacterial
structure-activity relationship
