在细菌感染小鼠模型中具有体内疗效的DNA结合配体：内部芳香族氨基酸的优化
DNA binding ligands with in vivo efficacy in murine models of bacterial infection: optimization of internal aromatic amino acids.
作者信息
Bürli Roland W, Kaizerman Jacob A, Duan Jian-Xin, Jones Peter, Johnson Kirk W, Iwamoto Mari, Truong Kiet, Hu Wenhao, Stanton Timothy, Chen Alfred, Touami Sofia, Gross Matthew, Jiang Vernon, Ge Yigong, Moser Heinz E
机构信息
Genesoft Pharmaceuticals, 7300 Shoreline Court, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2067-72. doi: 10.1016/j.bmcl.2004.02.047.
DNA binding ligands with potent antimicrobial activity against Gram-positive bacteria were further optimized by variation of the internal aromatic amino acids. This modification led to compounds with improved in vivo efficacy in lethal murine models of peritonitis (methicillin-resistant S. aureus, MRSA) and lung infection (S. pneumoniae).
通过改变内部芳香族氨基酸，对具有强效抗革兰氏阳性菌活性的DNA结合配体进行了进一步优化。这种修饰产生了在腹膜炎致死小鼠模型（耐甲氧西林金黄色葡萄球菌，MRSA）和肺部感染（肺炎链球菌）中体内疗效得到改善的化合物。
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