Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo
文献类型：期刊论文
| 作者 | Ni, Shuaishuai1; Wei, Hanwen1; Li, Baoli1; Chen, Feifei2; Liu, Yifu1; Chen, Wenhua1; Xu, Yixiang1; Qiu, Xiaoxia1; Li, Xiaokang1; Lu, Yanli1 |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2017-10-12 |
| 卷号 | 60期号:19页码:8145-8159 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/acs.jmedchem.7b00949 |
| 文献子类 | Article |
| 英文摘要 | Our previous work (Wang et al. J. Med. Chem. 2016, 59, 4831-4848) revealed that effective benzocycloalkane-derived staphyloxanthin inhibitors against methicillin-resistant Staphylococcus aureus (S. aureus) infections were accompanied by poor water solubility and high hERG inhibition and dosages (preadministration). In this study, 92 chroman and coumaran derivatives as novel inhibitors have been addressed for overcoming deficiencies above. Derivatives 69 and 105 displayed excellent pigment inhibitory activities and low hERG inhibition, along with improvement of solubility by salt type selection. The broad and significantly potent antibacterial spectra of 69 and 105 were displayed first with normal administration in the livers and hearts in mice against pigmented S. aureus Newman, Mu50 (vancomycin-intermediate S. aureus), and NRS271 (linezolid-resistant S. aureus), compared with linezolid and vancomycin. In summary, both 69 and 105 have the potential to be developed as good antibacterial candidates targeting virulence factors. |
| WOS关键词 | DIAPOPHYTOENE DESATURASE CRTN ; COMMUNITY-ASSOCIATED MRSA ; RISK-FACTORS ; BIOSYNTHESIS ; DISCOVERY ; EPIDEMIC |
| 资助项目 | National Natural Science Foundation of China[21672064] ; National Key R&D Program of China[2017YFB0-202600] ; Shanghai Municipal Education Commission[00000000] ; Shanghai Education Development Foundation[14SG28] ; Fundamental Research Funds for the Central Universities[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:000413131400014 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272453]  |
| 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 | 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,Wei, Hanwen,Li, Baoli,et al. Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo[J]. JOURNAL OF MEDICINAL CHEMISTRY,2017,60(19):8145-8159. |
| APA | Ni, Shuaishuai.,Wei, Hanwen.,Li, Baoli.,Chen, Feifei.,Liu, Yifu.,...&Li, Jian.(2017).Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.JOURNAL OF MEDICINAL CHEMISTRY,60(19),8145-8159. |
| MLA | Ni, Shuaishuai,et al."Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo".JOURNAL OF MEDICINAL CHEMISTRY 60.19(2017):8145-8159. |
入库方式： OAI收割
来源：上海药物研究所
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