当前位置：
X-MOL 学术
›
ACS Med. Chem. Lett.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-02-22 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00501 Shuaishuai Ni 1 , Baoli Li 1 , Feifei Chen 2 , Hanwen Wei 1 , Fei Mao 1 , Yifu Liu 1 , Yixiang Xu 1 , Xiaoxi Qiu 1 , Xiaokang Li 1 , Wenwen Liu 1 , Linghao Hu 1 , Dazheng Ling 1 , Manjiong Wang 1 , Xinyu Zheng 1 , Jin Zhu 1 , Lefu Lan 2 , Jian Li 1
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-02-22 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00501 Shuaishuai Ni 1 , Baoli Li 1 , Feifei Chen 2 , Hanwen Wei 1 , Fei Mao 1 , Yifu Liu 1 , Yixiang Xu 1 , Xiaoxi Qiu 1 , Xiaokang Li 1 , Wenwen Liu 1 , Linghao Hu 1 , Dazheng Ling 1 , Manjiong Wang 1 , Xinyu Zheng 1 , Jin Zhu 1 , Lefu Lan 2 , Jian Li 1
Affiliation
|
Diapophytoene desaturase (CrtN) is a potential novel target for intervening in the biosynthesis of the virulence factor staphyloxanthin. In this study, 38 1,4-benzodioxan-derived CrtN inhibitors were designed and synthesized to overwhelm the defects of leading compound 4a. Derivative 47 displayed superior pigment inhibitory activity, better hERG inhibitory properties and water solubility, and significantly sensitized MRSA strains to immune clearance in vitro. Notably, 47 displayed excellent efficacy against pigmented S. aureus Newman, Mu50 (vancomycin-intermediate MRSA, VISA), and NRS271 (linezolid-resistant MRSA, LRSA) comparable to that of linezolid and vancomycin in vivo.
中文翻译：
新型葡萄黄素抑制剂对多药耐药金黄色葡萄球菌具有增强的效力
番茄红素去饱和酶（CrtN）是干预毒力因子葡萄黄素生物合成的潜在新靶标。在这项研究中，设计并合成了38种1,4-苯并二恶烷衍生的CrtN抑制剂，以克服主要化合物4a的缺陷。衍生物47显示出优异的色素抑制活性，更好的hERG抑制特性和水溶性，并使MRSA菌株对体外免疫清除显着敏感。值得注意的是，与体内利奈唑胺和万古霉素相比，有47种药物对金黄色葡萄球菌纽曼，Mu50（万古霉素中间体MRSA，VISA）和NRS271（耐利奈唑胺的MRSA，LRSA）显示出优异的疗效。
更新日期：2018-02-22
中文翻译：
新型葡萄黄素抑制剂对多药耐药金黄色葡萄球菌具有增强的效力
番茄红素去饱和酶（CrtN）是干预毒力因子葡萄黄素生物合成的潜在新靶标。在这项研究中，设计并合成了38种1,4-苯并二恶烷衍生的CrtN抑制剂，以克服主要化合物4a的缺陷。衍生物47显示出优异的色素抑制活性，更好的hERG抑制特性和水溶性，并使MRSA菌株对体外免疫清除显着敏感。值得注意的是，与体内利奈唑胺和万古霉素相比，有47种药物对金黄色葡萄球菌纽曼，Mu50（万古霉素中间体MRSA，VISA）和NRS271（耐利奈唑胺的MRSA，LRSA）显示出优异的疗效。
京公网安备 11010802027423号