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由于喹诺酮类药物(如图1之结构式1所示)抗菌活性强,且口服有效,而引起人们极大的兴趣。然而,当许多优秀抗菌剂被开发(图1)的同时,只发表了少数几篇有关构效关系的文章。一般认为6位氟取代是所有最强抗菌剂的共同特点。对许多R_7取代物进行研究,活性变化较大,然而,Koga,Matsumoto及作者的系统研究清楚表明,R_7为五员或六员环时活性较好。关于R_8的研究很少。喹诺酮类的早期发展阶段,对1位为低级烷基及简单芳基取代的许多化合物进行了研
Quinolones, as shown in structural formula 1 of Figure 1, are of great interest due to their strong antibacterial activity and their effectiveness orally. However, while many excellent antibacterials have been developed (Figure 1), only a few articles on the structure-activity relationship have been published. It is generally accepted that the 6 fluorine substitution is a common feature of all the strongest antibacterials. However, the systematic studies by Koga, Matsumoto and the author made it clear that R_7 is more active when used as a five- or six-membered ring. There is little research on R_8. Quinolones of the early stages of development, one of the lower alkyl and simple aryl substituted many compounds were studied