| Summary: | 碩士 === 高雄醫學大學 === 藥學研究所碩士在職專班 === 94 === Recently, emergence of bacterial resistance to most common antimicrobial drugs such as ??ß-lactam antibiotics and macrolides is becoming a serious threat to worldwide public health. Introduction of fluoroquinolones such as norfloxacin and ciprofloxacin provided a valuable weapon against bacteria due to their unique mode of action, inhibition of bacterial DNA gyrase, and their favorable pharmacokinetic and safety profiles. Synthesis of new fluoroquinolones and the evaluation of these agents for antibacterial activity have continued and a series of SAR studies has been performed. However, the structural modification of the fluoroquinolones with respect to their optimum antibacterial activity has not been thoroughly explored. As part of our studies to improve antibacterial potency of fluoroquinolones especially their activities against resistant strains and M. tuberculosis, certain 7-substituted norfloxacin derivatives were synthesized for evaluation.
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