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靶向耐药革兰氏阳性菌的DNA结合配体。第1部分:内源性苯并咪唑衍生物。

DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives.

作者信息

Bürli Roland W, McMinn Dustin, Kaizerman Jacob A, Hu Wenhao, Ge Yigong, Pack Quinn, Jiang Vernon, Gross Matthew, Garcia Martin, Tanaka Richard, Moser Heinz E

机构信息

Genesoft Pharmaceuticals Inc., 7300 Shoreline Court, South San Francisco, CA 94080, USA.

出版信息

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1253-7. doi: 10.1016/j.bmcl.2003.12.042.

DOI:10.1016/j.bmcl.2003.12.042
PMID:14980676
Abstract

Novel DNA minor-groove binding ligands with a promising antibacterial profile are described. Apart from excellent in vitro potency against multiple Gram-positive bacterial strains such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecalis (VRE), and penicillin-intermediate Streptococcus pneumoniae (PISP), a small subset of compounds was active against Gram-negative bacteria such as Escherichia coli (E. coli).

摘要

描述了具有良好抗菌特性的新型DNA小沟结合配体。除了对多种革兰氏阳性细菌菌株,如耐甲氧西林金黄色葡萄球菌(MRSA)、耐万古霉素粪肠球菌(VRE)和青霉素中介肺炎链球菌(PISP)具有优异的体外活性外,一小部分化合物对革兰氏阴性细菌,如大肠杆菌(E. coli)也有活性。

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