Synthesis and antibacterial activity of 7-(3-amino-4-alkoxyimino-1 -piperidyl) -quinolones / 药学学报
Acta Pharmaceutica Sinica
; (12): 819-827, 2008.
Article
em Zh
| WPRIM
| ID: wpr-277771
Biblioteca responsável:
WPRO
ABSTRACT
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(-1) and 0.125 - 1 mg x L(-1), to S. epidermidis strains were 0.5 - 4 mg x L(-1) and 1 - 8 mg x L(-1) respectively. The in vivo results showed that they have as good internal protection as gemifloxacin and moxifloxacin against systemic infection model in mice (P > 0.05).
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Base de dados:
WPRIM
Assunto principal:
Farmacologia
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Infecções Pneumocócicas
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Infecções Estafilocócicas
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Estrutura Molecular
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Testes de Sensibilidade Microbiana
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Distribuição Aleatória
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Quinolonas
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Usos Terapêuticos
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Tratamento Farmacológico
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Staphylococcus aureus Resistente à Meticilina
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2008
Tipo de documento:
Article