Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators
文献类型：期刊论文
| 作者 | Kong, Xue-Qing1,2; Wei, Bing-Yan1,2; Yu, Chen-Xi1,2; Guan, Xiang-Na1,2; Ma, Wei-Ping1; Liu, Gang1; Yang, Cai-Guang1 ; Nan, Fa-Jun1,3
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| 刊名 | CHINESE JOURNAL OF CHEMISTRY
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| 出版日期 | 2020-07-01 |
| 页码 | 5 |
| ISSN号 | 1001-604X |
| DOI | 10.1002/cjoc.202000133 |
| 通讯作者 | Nan, Fa-Jun(fjnan@simm.ac.cn) |
| 英文摘要 | A Summary of main observation and conclusion To combat multidrug-resistant Gram-positive bacteria, new antimicrobials particularly those with novel mechanism of action are badly needed. Different with conventional antibiotics which are typical inhibitors, small-molecule activators of bacterial ClpP represent a new class of antibiotics. No ClpP activator has been developed for clinical trial. Herein, we conducted a screening on our library of bengamide-like ring-opened analogues and found that L472-2 possesses a low minimum inhibitory concentration (MIC) against S.aureus and shows no activity for ClpP activation in vitro, but it displayed reduced antibacterial activity against S. aureus with clpP deletion. In order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity, we perform further structural modifications starting from L472-2. Compound 37 remains the antimicrobial activity and activation of ClpP protein in vitro, which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation. |
| 资助项目 | Science and Technology Commission Shanghai Municipality[16ZR1407000] ; Science and Technology Commission Shanghai Municipality[17XD1404400] ; National Natural Science Foundation of China[81861138046] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000544601600001 |
| 出版者 | WILEY-V C H VERLAG GMBH |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/291847]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Nan, Fa-Jun |
| 作者单位 | 1.Chinese Acad Sci, Chinese Natl Ctr Drug Screening, CAS Key Lab Receptor Res, State Key Lab Drug Res,Shanghai Inst Mat Med, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Yantai Inst Mat Med, Yantai Key Lab Nanomed & Adv Preparat, 39 Sci & Technol Ave, Yantai 264000, Shandong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Kong, Xue-Qing,Wei, Bing-Yan,Yu, Chen-Xi,et al. Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators[J]. CHINESE JOURNAL OF CHEMISTRY,2020:5. |
| APA | Kong, Xue-Qing.,Wei, Bing-Yan.,Yu, Chen-Xi.,Guan, Xiang-Na.,Ma, Wei-Ping.,...&Nan, Fa-Jun.(2020).Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators.CHINESE JOURNAL OF CHEMISTRY,5. |
| MLA | Kong, Xue-Qing,et al."Design, Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators".CHINESE JOURNAL OF CHEMISTRY (2020):5. |
入库方式： OAI收割
来源：上海药物研究所
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