Synthesis and antibacterial activity of dl-7-(4,4-dimethyl-3-aminomethylpyrrolidinyl) -quinolones.
- Author:
Yu-Cheng WANG
1
;
Xiu-Yun WANG
;
Jiu-Yu LIU
;
Hui-Yuan GUO
Author Information
- Publication Type:Journal Article
- MeSH: Anti-Bacterial Agents; chemical synthesis; pharmacology; Gram-Negative Aerobic Bacteria; drug effects; Gram-Positive Bacteria; drug effects; Microbial Sensitivity Tests; Molecular Structure; Pseudomonas aeruginosa; drug effects; Quinolones; chemical synthesis; pharmacology; Staphylococcus epidermidis; drug effects
- From: Acta Pharmaceutica Sinica 2006;41(1):58-64
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo explore new agents of quinolone derivatives with high activity against Gram-positive organisms.
METHODSdl-7-(4,4-Dimethyl-3- aminomethylpyrrolidinyl)-quinolones were designed and synthesized, and their activity against Gram-positive organisms was tested in vitro.
RESULTSTen 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)).
CONCLUSIONThe compound 22 showed high activity against Gram-positive organisms in vitro and it is worth of more investigation.
