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为寻找新的喹诺酮类抗菌药,设计合成了16个7-(3-甲基-3-甲胺基-4-烷氧亚胺基-1-哌啶基)喹诺酮类化合物,并测定其体外抗菌活性。目标化合物结构经1HNMR和HRMS得到确证,并用单晶X-衍射分析确定其双键构型。化合物14k和14m～14o对所试验的5株革兰阳性菌和5株革兰阴性菌表现出良好的广谱抗菌活性(MIC:0.25～16μg·mL-1),其中活性最强的化合物14o对金葡菌、表葡菌、粪肠球菌和大肠埃希菌的活性(MIC:0.25～1μg·mL-1)与左氧氟沙星相当,对肺炎链球菌的活性(MIC:4μg·mL-1)是左氧氟沙星的8倍,但总体上弱于吉米沙星。
In order to find new quinolone antibacterials, 16 compounds of 7- (3-methyl-3-methylamino-4-alkoxyimino-1-piperidinyl) quinolones were designed and synthesized, and their in vitro Antibacterial activity. The structure of the target compound was confirmed by 1HNMR and HRMS and its double bond configuration was confirmed by single crystal X-ray diffraction. Compounds 14k and 14m ~ 14o showed good broad-spectrum antibacterial activity (MIC: 0.25 ~ 16μg · mL-1) against 5 Gram-positive bacteria and 5 Gram-negative bacteria tested. The most active compounds were 14o The activity against S.aureus, S.epivoxil, E. faecalis and E.coli (MIC: 0.25-1 μg · mL-1) was comparable to that of levofloxacin, and the activity against S. pneumoniae (MIC: 4 μg · mL -1) was Levofloxacin 8 times, but overall weaker than gemifloxacin.