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1962年,Lesher 等首先报道了一类全新的抗菌药物——萘啶酸。1977年,Albrecht就有关萘啶酸类抗菌药的构效关系、抗菌活性以及化学合成进行了较全面的综述。自1977年以来,已报道合成了6000多个该类类似化合物,其中大约有20个现已成为药物上市或正处于深入开发中。1980年由 Koga等报道了较萘啶酸活性更加优越的诺氟沙星,它成为氟喹诺酮类药物的代表,而后文献大量报道了该类结构改造工作。本文主要就新氟喹诺酮化学进展作一总结。
In 1962, Lesher first reported a class of new antibacterial drugs - nalidixic acid. In 1977, Albrecht conducted a comprehensive review on the structure-activity relationship, antimicrobial activity and chemical synthesis of nalidixic acid antibacterials. Since 1977, it has been reported that more than 6,000 such similar compounds have been synthesized, of which about 20 are now drug-listed or in-depth development. In 1980, Koga et al. Reported that norfloxacin was more superior to nalidixic acid and became a representative of fluoroquinolones. Then, a large number of reports on the structural remodeling work have been reported in the literature. This paper mainly summarizes the chemical progress of new fluoroquinolones.