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Novel membrane-targeting isoxanthohumol-amine conjugates for combating methicillin-resistant Staphylococcus aureus (MRSA) infections

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成果类型:
期刊论文
作者:
Yang, Ruige;Cheng, Wanqing;Huang, Meijuan;Xu, Ting;Zhang, Miaomiao;...
通讯作者:
Guo, Y
作者机构:
[Yang, Ruige; Guo, Yong; Guo, Y; Xu, Ting] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Sch Pharmaceut Sci, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.
[Yang, Ruige; Zhang, Miaomiao; Cheng, Wanqing; Huang, Meijuan; Liu, Jifeng; Guo, Yong; Qin, Shangshang] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China.
通讯机构:
[Guo, Y ] U
Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Sch Pharmaceut Sci, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.
语种:
英文
关键词:
Antibacterial activity;Bacterial resistance;Isoxanthohumol-amine conjugate;Membrane-targeting mode;Methicillin-resistant Staphylococcus aureus
期刊:
European Journal of Medicinal Chemistry
ISSN:
0223-5234
年:
2024
卷:
268
页码:
116274
基金类别:
CRediT authorship contribution statement Ruige Yang: Writing – original draft, Data curation, Conceptualization. Wanqing Cheng: Methodology, Investigation. Meijuan Huang: Methodology. Ting Xu: Data curation. Miaomiao Zhang: Investigation. Jifeng Liu: Conceptualization. Shangshang Qin: Supervision, Conceptualization. Yong Guo: Writing – review & editing, Supervision, Project administration, acquisition, Conceptualization.
机构署名:
本校为第一且通讯机构
摘要:
Methicillin-resistant Staphylococcus aureus (MRSA) is a widespread pathogen causing clinical infections and is multi-resistant to many antibiotics, making it urgent need to develop novel antibacterials to combat MRSA. Here, a series of novel isoxanthohumol-amine conjugates were synthesized as antibacterials. After bioactivity evaluation, a compound E2 was obtained, which showed excellent antibacterial activity against S. aureus and clinical MRSA isolates (MICs=0.25-1μg/mL), superior to vancomycin, and with negligible hemolysis and good membran...

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