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Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents

文献类型：期刊论文

作者Zhong, Yuanchen1,4; Liu, Huan2,3,4; Chen, Feifei2,3,4; He, Qian4; Zhang, Xiaofei4; Lan, Lefu2,3; Yang, Chunhao2,4
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2024-03-15
卷号268页码:9
关键词Pyrrolomycin analogues Antibacterial agents Anti-biofilm Drug -resistant bacteria Thiazole
ISSN号0223-5234
DOI10.1016/j.ejmech.2024.116221
通讯作者Zhang, Xiaofei(xiaofeizhang@simm.ac.cn) ; Lan, Lefu(llan@ucas.ac.cn) ; Yang, Chunhao(chyang@simm.ac.cn)
英文摘要The formation of biofilm is one of the important factors for bacteria to develop drug-resistant. A series of halogenated-pyrroles or pyrazoles containing thiazole groups as antibacterial agents were designed and synthesized to target biofilms. Among them, compound 8c showed antibacterial activity against various Grampositive bacteria, particularly against vancomycin-resistant Enterococcus faecalis (MIC <= 0.125 mu g/mL). Additionally, this compound significantly inhibited biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa at sub-MIC doses. Furthermore, compound 8c exhibited significantly lower mammalian cell toxicity compared to pyrrolomycin C and its hepatic microsomal metabolic stability in various species was also evaluated. Further experiment on the infection model of Galleria mellonella proved that the compound was effective in vivo.
WOS关键词ANTI-BIOFILM ACTIVITY
资助项目National Natural Science Foundation of China (NSFC)[21907104] ; Research Funds of Hangzhou Institute for Advanced Study, UCAS[2023HIAS- V006] ; National Key Research and Development Program of China[2023YFD1800102]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001188894900001
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
源URL[http://119.78.100.183/handle/2S10ELR8/310354]  
专题新药研究国家重点实验室
通讯作者Zhang, Xiaofei; Lan, Lefu; Yang, Chunhao
作者单位1.Shanghai Univ, Dept Chem, Shanghai 200444, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zhong, Yuanchen,Liu, Huan,Chen, Feifei,et al. Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2024,268:9.
APA Zhong, Yuanchen.,Liu, Huan.,Chen, Feifei.,He, Qian.,Zhang, Xiaofei.,...&Yang, Chunhao.(2024).Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,268,9.
MLA Zhong, Yuanchen,et al."Design, synthesis and biological evaluation of thiazolyl-halogenated pyrroles or pyrazoles as novel antibacterial and antibiofilm agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 268(2024):9.

入库方式： OAI收割

来源：上海药物研究所

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