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首页> 外文期刊>Antimicrobial agents and chemotherapy. >In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
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In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.

机译:三种新型二氢叶酸还原酶抑制剂对革兰氏阳性细菌临床分离株的体外活性。

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摘要

BAL0030543, BAL0030544, and BAL0030545 are dihydrophthalazine inhibitors with in vitro potency against gram-positive pathogens. The MIC(50)s for methicillin (meticillin)-sensitive Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, hetero-vancomycin-resistant Staphylococcus aureus, and vancomycin-resistant Staphylococcus aureus (VISA) range from 0.015 to 0.25 microg/ml (MIC(90)s < or = 0.5 microg/ml). MIC(50)s for beta-hemolytic streptococci range from 0.03 to 0.06 microg/ml, MIC(50)s for Streptococcus pneumoniae range from 0.06 to 0.12 microg/ml, MIC(50)s for Listeria monocytogenes range from 0.015 to 0.06 microg/ml, and MIC(50)s for Streptococcus mitis are < or = 0.015 microg/ml. These three dihydrophthalazine antifolates have improved potency compared to that of trimethoprim and activity against gram-positive pathogens resistant to other drug classes. (This work was presented in part at the 48th Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington, DC, 2008.).
机译:BAL0030543,BAL0030544和BAL0030545是二氢酞嗪抑制剂,对革兰氏阳性病原体具有体外效力。甲氧西林(美西林)敏感的金黄色葡萄球菌,耐甲氧西林的金黄色葡萄球菌,耐万古霉素的金黄色葡萄球菌和耐万古霉素的金黄色葡萄球菌(VISA)的MIC(50)范围为0.015至0.25 microg / ml(MIC( 90)s <或= 0.5 microg / ml)。 β-溶血性链球菌的MIC(50)范围为0.03至0.06微克/毫升,肺炎链球菌的MIC(50)范围为0.06至0.12微克/毫升,单核细胞增生李斯特菌的MIC(50)范围为0.015至0.06微克/ ml,而链球菌的MIC(50)≤0.015 microg / ml。与甲氧苄氨嘧啶相比,这三种二氢酞嗪抗叶酸剂的功效有所提高,并且具有抗其他药物类别的革兰氏阳性病原体的活性。 (这项工作在第48届抗菌药物与化学间科学大会上作了部分介绍,华盛顿特区,2008年。)

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