Synthesis and antibacterial activity of 7-(3-amino-4-alkoxyimino-1 -piperidyl) -quinolones

• Published in: Yao hsüeh hsüeh pao Vol. 43; no. 8; p. 819
• Main Authors: Wang, Xiu-Yun, Guo, Qiang, Wang, Yu-Cheng, Liu, Bing-Quan, Liu, Ming-Liang, Sun, Lan-Ying, Guo, Hui-Yuan
• Format: Journal Article
• Language: Chinese
• Published: China 01.08.2008
• Subjects: Animals; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - pharmacology; Anti-Bacterial Agents - therapeutic use; Female; Gram-Negative Bacteria - drug effects; Gram-Positive Bacteria - drug effects; Male; Methicillin-Resistant Staphylococcus aureus - drug effects; Mice; Microbial Sensitivity Tests; Molecular Structure; Pneumococcal Infections - drug therapy; Quinolones - chemical synthesis; Quinolones - pharmacology; Quinolones - therapeutic use; Random Allocation; Staphylococcal Infections - drug therapy
• ISSN: 0513-4870

To explore new agents of quinolone derivatives with high activity against Gram-positive and Gram-negative microorganisms, 7-(3-amino-4-alkoxyimino-1-piperidyl) quinolones were designed and synthesized, and their activity against Gram-positive and Gram- negative microorganisms were tested in vivo and in vitro. Twenty one target compounds were obtained. Their structures were established by 1H NMR, HRMS and X-ray crystallographic analysis. The target compounds possess different antimicrobial activities against both Gram-negative and Gram-positive microorganisms. Compounds 14a and 14m have broad spectral antibacterial activities. They show better antibacterial activities against 12 strains Gram-positive bacteria than three references. In particular, their activities against S. aureus and S. epidermidis (including MRSA and MRSE) were 4 - 16 times than that of gemifloxacin and balofloxacin, and 8 - 64 times than that of levofloxacin. The MIC values to S. aureus strains of compounds 14a and 14m were 0.25 - 1 mg x L(