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

doi:10.1002/cjoc.202000502

	Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus(dagger)
	Yu, Chen-Xi 3,4; Wei, Bing-Yan 1,3; Kong, Xue-Qing 3,4; Yang, Cai-Guang 1,3,4; Nan, Fa-Jun 2,3,4
刊名	CHINESE JOURNAL OF CHEMISTRY
	2021-03-01
卷号	39 期号:3 页码:671-676
关键词	Bengamides Staphylococcus aureus Antibiotics Structure‐ activity relationships Pharmacokinetic
ISSN号	1001-604X
DOI	10.1002/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
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/295577]
专题	中国科学院上海药物研究所
通讯作者	Yang, Cai-Guang; Nan, Fa-Jun
作者单位	1.UCAS, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Zhejiang, Peoples R China 2.Yantai Inst Mat Med, Yantai Key Lab Nanomed & Amp Adv Preparat, Yantai 264000, Shandong, Peoples R China 3.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, 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.