RESUMO
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).
Assuntos
Animais , Feminino , Masculino , Camundongos , Antibacterianos , Farmacologia , Usos Terapêuticos , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Staphylococcus aureus Resistente à Meticilina , Testes de Sensibilidade Microbiana , Estrutura Molecular , Infecções Pneumocócicas , Tratamento Farmacológico , Quinolonas , Farmacologia , Usos Terapêuticos , Distribuição Aleatória , Infecções Estafilocócicas , Tratamento FarmacológicoRESUMO
OBJECTIVE@#To improve DNA extraction from bloodstain on the filter paper and to establish a rapid, simple, and cost-effective method for DNA extraction suitable for database construction.@*METHODS@#Seven hundred and fifty two aged bloodstains on filter paper were randomly divided into four groups. The four different DNA extraction methods were compared with each other, and two DNA extraction methods used for 63 fresh bloodstains on filter paper were also compared with each other.@*RESULTS@#There were no statistically significant differences observed among the four DNA extraction methods (P > 0.05) for aged bloodstains on filter paper; But the difference between the two DNA extraction methods for fresh bloodstains on filter paper was obviously (P < 0.05).@*CONCLUSION@#Extraction of DNA samples from aged bloodstains on filter paper can be accomplished by using Chlex-100 methodology directly with no need to wash the bloodstains.