Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus
文献类型：期刊论文
| 作者 | Ni, Shuaishuai1; Li, Baoli1; Chen, Feifei2; Wei, Hanwen1; Mao, Fei1; Liu, Yifu1; Xu, Yixiang1; Qiu, Xiaoxi1; Li, Xiaokang1; Liu, Wenwen1 |
| 刊名 | ACS MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2018-03 |
| 卷号 | 9期号:3页码:233-237 |
| 关键词 | Virulence factor pigment multidrug resistant MRSA CrtN inhibitor |
| ISSN号 | 1948-5875 |
| DOI | 10.1021/acsmedchemlett.7b00501 |
| 文献子类 | Article |
| 英文摘要 | 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. |
| WOS关键词 | DIAPOPHYTOENE DESATURASE CRTN ; METHICILLIN-RESISTANT ; LINEZOLID-RESISTANT ; VIRULENCE FACTOR ; MRSA INFECTIONS ; IN-VIVO ; BIOSYNTHESIS ; VANCOMYCIN ; TOLERANCE ; DISCOVERY |
| 资助项目 | National Key R&D Program of China[2017YFB0202600] ; National Natural Science Foundation of China[21672064] ; "Shu Guang" project - Shanghai Municipal Education Commission[00000000] ; Shanghai Education Development Foundation[14SG28] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000427331200012 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279872]  |
| 专题 | 药理学第三研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Zhu, Jin; Lan, Lefu; Li, Jian |
| 作者单位 | 1.East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ni, Shuaishuai,Li, Baoli,Chen, Feifei,et al. Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus[J]. ACS MEDICINAL CHEMISTRY LETTERS,2018,9(3):233-237. |
| APA | Ni, Shuaishuai.,Li, Baoli.,Chen, Feifei.,Wei, Hanwen.,Mao, Fei.,...&Li, Jian.(2018).Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus.ACS MEDICINAL CHEMISTRY LETTERS,9(3),233-237. |
| MLA | Ni, Shuaishuai,et al."Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant Staphylococcus aureus".ACS MEDICINAL CHEMISTRY LETTERS 9.3(2018):233-237. |
入库方式： OAI收割
来源：上海药物研究所
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