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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。
Objective To find quinolone anti-TB drugs with excellent activity. Methods Gatifloxacin derivatives containing substituted indolin-1-ethyl were synthesized and synthesized. The antimycobacterial activity in vitro was determined. Results A total of 14 new compounds were synthesized and their structures were confirmed by 1H-NMR, MS and HRMS. The target generally has good anti-mycobacterial activity (MIC of 1.56 ~ 6.25μg / mL), but are weaker than its parent drug gatifloxacin. Among them, the activity of compound 3h against Mycobacterium phlei CMCC93201 and Mycobacterium smegmatis CMCC93202 was 4-fold and 2-fold higher than that of rifampin, respectively. Conclusion Liposolubility is not the only factor that determines the anti-mycobacterial activity of quinolones.