中国抗生素杂志
中國抗生素雜誌
중국항생소잡지
CHINESE JOURNAL OF ANTIBIOTICS
2011年
1期
37-43
,共7页
万志龙%刘明亮%冯连顺%王博%郑旭东%郭慧元
萬誌龍%劉明亮%馮連順%王博%鄭旭東%郭慧元
만지룡%류명량%풍련순%왕박%정욱동%곽혜원
加替沙星衍生物%合成%抗分枝杆菌活性
加替沙星衍生物%閤成%抗分枝桿菌活性
가체사성연생물%합성%항분지간균활성
Gatifloxacin derivatives%Synthesis%Antimycobacterial activity
目的 寻找具有优秀活性的喹诺酮类抗结核药物.方法 设计合成脂溶性更大的含有取代吲哚满二酮-1-乙基的加替沙星衍生物,测定其体外抗分枝杆菌活性.结果 共合成了14个新化合物,其结构经1H-NMR、MS和HRMS确证.目标物普遍具有良好的抗分枝杆菌活性(MIC为1.56～6.25μg/mL),但均弱于其母药加替沙星.其中,化合物3h对草分枝杆菌CMCC93201和耻垢分枝杆菌CMCC93202的活性分别是利福平的4倍和2倍.结论 脂溶性并非决定喹诺酮类化合物抗分枝杆菌活性的唯一因素.
目的 尋找具有優秀活性的喹諾酮類抗結覈藥物.方法 設計閤成脂溶性更大的含有取代吲哚滿二酮-1-乙基的加替沙星衍生物,測定其體外抗分枝桿菌活性.結果 共閤成瞭14箇新化閤物,其結構經1H-NMR、MS和HRMS確證.目標物普遍具有良好的抗分枝桿菌活性(MIC為1.56～6.25μg/mL),但均弱于其母藥加替沙星.其中,化閤物3h對草分枝桿菌CMCC93201和恥垢分枝桿菌CMCC93202的活性分彆是利福平的4倍和2倍.結論 脂溶性併非決定喹諾酮類化閤物抗分枝桿菌活性的唯一因素.
목적 심조구유우수활성적규낙동류항결핵약물.방법 설계합성지용성경대적함유취대신타만이동-1-을기적가체사성연생물,측정기체외항분지간균활성.결과 공합성료14개신화합물,기결구경1H-NMR、MS화HRMS학증.목표물보편구유량호적항분지간균활성(MIC위1.56～6.25μg/mL),단균약우기모약가체사성.기중,화합물3h대초분지간균CMCC93201화치구분지간균CMCC93202적활성분별시리복평적4배화2배.결론 지용성병비결정규낙동류화합물항분지간균활성적유일인소.
Objective To find new anti-tuberculosis agents of quinolones with high activity. Methods A series of novel gatifloxacin ethylene isatin derivatives possessing more lipophilicity were designed, synthesized and evaluated for their in vitro activity against mycobacteria. Results Fourteen new compounds were obtained and characterized by 1H-NMR, MS and HRMS. These derivatives have considerable activity against the tested two strains (MIC1.56~6.25μg/mL), although less active than the parent drug gatifloxacin. Compound 3h was 4-fold and 2-fold more potent than rifampin against M. phlei CMCC 93201 and M. smegmatis CMCC 93202, respectively. Conclusion The lipophilicity of the new compounds is not the sole parameter affecting antimycobacterial activity.
