Synthesis of Quinolone Benzimidazoles As Topoisomerase Inhibitors

来源 :中国化学会全国第十二届有机合成化学学术研讨会 | 被引量 : 0次 | 上传用户:yuandatoy
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  Synthesis of topoisomerases inhibitors has earned considerable interest in medicinal chemistry as they are able to catalyze changes in DNA topology and are clinically validated targets for antibacterial drug discovery.Benzimidazoles and quinolones were revealed to important kind of important topoisomerase inhibitors.The development of quinolone benzimidazole derivatives as novel antibacterial agents may be served as a good strategy to exploit new anti-infective agents with better activity and less bacterial resistances.Herein we developed a series of novel fluoroquinolone-based benzimidazoles with various types of linkers including-CH2-,-CH2-CH2-,-CH2-NH-and shiffbase(-C=N-)ones,as well as the spacers with different lengths of aliphatic chains.
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