Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus

doi:10.1016/j.ejmech.2020.112352

	Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus
	Wang, Zhi-Cheng 2; Wei, Bingyan 1,3; Pei, Fang-Ning 2; Yang, Teng 3,4; Tang, Jie 2; Yang, Song 4; Yu, Li-Fang 2; Yang, Cai-Guang 1,3; Yang, Fan 2
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	2020-07-15
卷号	198 页码:11
关键词	Capsaicin Nitrothiophene Multidrug-resistant S. aureus Antibacterial agent
ISSN号	0223-5234
DOI	10.1016/j.ejmech.2020.112352
通讯作者	Yang, Cai-Guang(yangcg@simm.ac.cn) ; Yang, Fan(fyang@chem.ecnu.edu.cn)
英文摘要	To address the emergency caused by multi-drug resistant Staphylococcus aureus, a series of novel capsaicin derivatives with nitrothiophene substituents have been designed and evaluated for the antibacterial activities against S. aureus Newman and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The structure-activity relationship was further revealed. Compound 13c, 13f, and 13g were highly active against staphylococcal growth, with minimal inhibition concentration (MIC) values of 0.39-1.56 mu g/mL. The oxadiazole-derived compound 21, a bioisostere of ester 13f, is the most potent candidate for anti-growth of five multidrug-resistant S. aureus strains with MICs of 0.20-0.78 mu g/mL, which is more active compared with vancomycin in vitro. Notably, these anti-staphylococcal compounds are much less cytotoxic to the normal kidney epithelial cell line (HK293T). (C) 2020 Elsevier Masson SAS. All rights reserved.
资助项目	National Key Technology RD Program[2015BAK45B00] ; National Natural Science Foundation of China[81861138046] ; Science and Technology Commission Shanghai Municipality[16DZ2280100] ; Science and Technology Commission Shanghai Municipality[17XD1404400] ; Laboratory of Organic Functional Molecules, Sino-French Institute of East China Normal University
WOS关键词	STAPHYLOCOCCUS-AUREUS ; ANTIMICROBIAL ACTIVITY ; 5-NITROTHIOPHENE ; ANTIBIOTICS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号	WOS:000539425800008
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/291676]
专题	中国科学院上海药物研究所
通讯作者	Yang, Cai-Guang; Yang, Fan
作者单位	1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, SCME, Shanghai 200062, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China 4.Guizhou Univ, Ctr R&D Fine Chem, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, 2708 South Huaxi Rd, Guiyang 550025, Guizhou, Peoples R China
推荐引用方式 GB/T 7714	Wang, Zhi-Cheng,Wei, Bingyan,Pei, Fang-Ning,et al. Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2020,198:11.
APA	Wang, Zhi-Cheng.,Wei, Bingyan.,Pei, Fang-Ning.,Yang, Teng.,Tang, Jie.,...&Yang, Fan.(2020).Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,198,11.
MLA	Wang, Zhi-Cheng,et al."Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 198(2020):11.