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Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger)

文献类型：期刊论文

作者Yu, Chen-Xi1,2; Wei, Bing-Yan1,3; Kong, Xue-Qing1,2; Yang, Cai-Guang1,2,3; Nan, Fa-Jun1,2,4
刊名CHINESE JOURNAL OF CHEMISTRY
出版日期2021-03-01
卷号39期号:3页码:671-676
ISSN号1001-604X
关键词Bengamides Staphylococcus aureus Antibiotics Structure‐ activity relationships Pharmacokinetic
DOI10.1002/cjoc.202000502
通讯作者Yang, Cai-Guang(yangcg@simm.ac.cn) ; Nan, Fa-Jun(fjnan@simm.ac.cn)
英文摘要Main observation and conclusion Methicillin-resistant Staphylococcus aureus (MRSA) has become a major threat on public health because of the increase of clinically isolated strains that exhibit resistance to many antibiotics. Therefore, development of new antibiotics for the treatment of MRSA infection is a sustained challenge. We have previously identified a ring-opened bengamide analogue L472-2 that displays moderate activity against the growth of S. aureus. In our previous work, we started from L472-2 and identified a class of analogues containing alkynyl groups which have the potential to activate SaClpP activity but moderate antibacterial activity. Herein, we focused on the antibacterial activity of L472-2, and a novel series of ring-opened bengamide analogues were synthesized and their activities were evaluated against MRSA. By conducting a compact analysis of the structure-activity relationships (SAR) of these analogues, we found that an adamantane ethanol ester bengamide 2j showed excellent antibacterial activity towards six S. aureus strains, including MRSA, while it does not activate ClpP. Therefore, these bengamide analogues represent a new class of candidates that suppress MRSA viability.
WOS研究方向Chemistry
语种英语
出版者WILEY-V C H VERLAG GMBH
WOS记录号WOS:000619567500021
源URL[http://119.78.100.183/handle/2S10ELR8/295577]  
专题新药研究国家重点实验室
通讯作者Yang, Cai-Guang; Nan, Fa-Jun
作者单位1.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.UCAS, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Zhejiang, Peoples R China
4.Yantai Inst Mat Med, Yantai Key Lab Nanomed & Amp Adv Preparat, Yantai 264000, Shandong, Peoples R China
推荐引用方式
GB/T 7714		 Yu, Chen-Xi,Wei, Bing-Yan,Kong, Xue-Qing,et al. Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger)[J]. CHINESE JOURNAL OF CHEMISTRY,2021,39(3):671-676.
APA Yu, Chen-Xi,Wei, Bing-Yan,Kong, Xue-Qing,Yang, Cai-Guang,&Nan, Fa-Jun.(2021).Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger).CHINESE JOURNAL OF CHEMISTRY,39(3),671-676.
MLA Yu, Chen-Xi,et al."Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger)".CHINESE JOURNAL OF CHEMISTRY 39.3(2021):671-676.

入库方式： OAI收割

来源：上海药物研究所

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