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  • Title: [Synthesis and antibacterial activity of dl-7-(4,4-dimethyl-3-aminomethylpyrrolidinyl) -quinolones].
    Author: Wang YC, Wang XY, Liu JY, Guo HY.
    Journal: Yao Xue Xue Bao; 2006 Jan; 41(1):58-64. PubMed ID: 16683529.
    Abstract:
    AIM: 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)). CONCLUSION: The compound 22 showed high activity against Gram-positive organisms in vitro and it is worth of more investigation.
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