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目的寻找新的喹诺酮类抗菌药。方法设计合成7-位具有较强亲水性取代基的7个氟喹诺酮衍生物,测定其体外抗菌活性。结果化合物10对金葡菌(包括MRSA)和表葡菌(包括MRSE)的活性(MIC:0.06~4μg/mL)与左氧氟沙星和吉米沙星基本相当。化合物11对肺炎链球菌08-2的活性(MIC:0.25μg/mL)分别是左氧氟沙星和吉米沙星的128倍和32倍,化合物12对肺炎克雷伯菌09-22和09-23的活性(MIC:1μg/mL)分别是左氧氟沙星和吉米沙星的16倍和4倍,但目标物对革兰阴性菌的活性普遍弱于对照药。结论 7-位取代基的水溶性并非决定喹诺酮抗菌活性的主要因素。
Aim To find new quinolone antibacterials. Methods Seven fluoroquinolone derivatives with strong hydrophilic substituents at the 7-position were designed and synthesized, and their antibacterial activities were determined in vitro. Results The activity of compound 10 against S. aureus (including MRSA) and S. epidermidis (including MRSE) (MIC: 0.06-4 μg / mL) was almost equivalent to that of levofloxacin and gemifloxacin. The activity of compound 11 against S. pneumoniae 08-2 (MIC: 0.25 μg / mL) was 128-fold and 32-fold higher for levofloxacin and gemifloxacin respectively. The activity of compound 12 against K. pneumoniae 09-22 and 09-23 (MIC: 1 μg / mL) were 16-fold and 4-fold higher for levofloxacin and gemifloxacin, respectively, but the activity of the target against Gram-negative bacteria was generally weaker than that of the reference drug. Conclusion The water-solubility of 7-substituent is not the main factor that determines the antibacterial activity of quinolone.