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目的:介绍氟喹诺酮类药物7位取代杂环的构效关系。方法:通过查阅国内外相关文献,对7位含二联氨结构的取代杂环的氟喹诺酮的多项药理学参数加以分析总结。结果:抗菌活性、口服生物利用度、光毒性、细胞毒性等药理学参数对评价该类化合物的研发价值具有指导作用。结论:C-7位含有氨基吡咯烷和氨基氮杂环丁烷等,均可提供较好的广谱抗菌活性。部分其他7位取代基也具有一定的研发价值。
Objective: To introduce the structure-activity relationship of 7-substituted heterocycle of fluoroquinolones. Methods: By referring to relevant literatures at home and abroad, a series of pharmacological parameters of fluoroquinolones containing 7 substituted heterocyclic rings containing dihydric ammonia structure were analyzed and summarized. Results: Pharmacological parameters such as antibacterial activity, oral bioavailability, phototoxicity and cytotoxicity were helpful to evaluate the R & D value of these compounds. Conclusion: C-7 contains aminopyrrolidine and amino-azetidine, etc., can provide good broad-spectrum antibacterial activity. Some of the other seven substituents also have some research and development value.