[Synthesis and antibacterial activity of dl-7-(4,4-dimethyl-3-aminomethylpyrrolidinyl) -quinolones].
OBJECTIVE
To explore new agents of quinolone derivatives with high activity against Gram-positive organisms.


METHODS
dl-7-(4,4-Dimethyl-3- aminomethylpyrrolidinyl)-quinolones were designed and synthesized, and their activity against Gram-positive organisms was tested in vitro.


RESULTS
Ten target compounds were obtained. The structures of these compounds were confirmed by 1H NMR, MS. The target compounds with dl-4,4-dimethyl-3-( methyl) aminomethylpyrrolidine side chains had high activity against Gram-positive organisms. Especially the MIC values of compound 22 for 4 strains of Gram-positive resistant bacteria (two strains of MRSA and two of MRSE) were 0.015 -0.5 mg x L(-), which exhibited more potent activities than gatifloxacin (4 - 128 times). Its MIC value for Pseudomonas aeruginosa 03-5 (0.008 mg x L(-1)) was 4 times as that of gatifloxacin (0.03 mg x L(-1)).


CONCLUSIONS
The compound 22 showed high activity against Gram-positive organisms in vitro and it is worth of more investigation.
Wang
Yu-Cheng
YC
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Wang
Xiu-Yun
XY
Liu
Jiu-Yu
JY
Guo
Hui-Yuan
HY