Mahboobi Siavosh, Eichhorn Emerich, Winkler Matthias, Sellmer Andreas, Möllmann Ute
Department of Pharmaceutical Chemistry I, University of Regensburg, D-93040 Regensburg, Germany.
Eur J Med Chem. 2008 Mar;43(3):633-56. doi: 10.1016/j.ejmech.2007.05.009. Epub 2007 Jun 3.
Compounds containing 3-bromo-2,5-dihydro-1H-2,5-pyrroledione and indole substructures were found to have antibacterial activity against resistant strains of Staphylococcus aureus and some other Gram positive bacteria. The investigated compounds exhibit minimal inhibition concentrations (MICs) lower than those of common antibiotics like vancomycin or ciprofloxacin. Activity against multiresistant strains suggests a mechanism of action different from common antibiotics. This might be important in circumventing existing resistance mechanisms. Here we report about the antibacterial activity in an extended structure-activity relationship study.
含有3-溴-2,5-二氢-1H-2,5-吡咯二酮和吲哚亚结构的化合物被发现对耐甲氧西林金黄色葡萄球菌及其他一些革兰氏阳性菌具有抗菌活性。所研究的化合物表现出的最低抑菌浓度（MIC）低于万古霉素或环丙沙星等常用抗生素。对多重耐药菌株的活性表明其作用机制不同于常用抗生素。这在规避现有耐药机制方面可能很重要。在此，我们在一项扩展的构效关系研究中报告了其抗菌活性。
