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Development of Membrane-Targeting Fluorescent 2-Phenyl-1H-phenanthro[9,10-d]imidazole-Antimicrobial Peptide Mimic Conjugates against Methicillin-Resistant Staphylococcus aureus

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成果类型:
期刊论文
作者:
Xu, Ting;Yan, Xiaoting;Kang, Ayue;Yang, Longhua;Li, Xinhui;...
通讯作者:
Yang, Ruige;Guo, Y;Qin, Shangshang
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; Qin, Shangshang; Kang, Ayue; Yan, Xiaoting; Yang, Longhua; Guo, Yong; Tian, Yue; Guo, Y; Li, Xinhui] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China.
通讯机构:
[Yang, RG; Guo, Y ] U
[Qin, SS] Z
Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Sch Pharmaceut Sci, Hengyang Med Sch, Hengyang 421001, Hunan, Peoples R China.
Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Henan, Peoples R China.
语种:
英文
期刊:
JOURNAL OF MEDICINAL CHEMISTRY
ISSN:
0022-2623
年:
2024
基金类别:
University of South China [231RGC014, 241RGC001]; Startup Research Fund from the University of South China [232301420097]; Science and Technology R&D Programme Joint Fund of Henan Province
机构署名:
本校为第一且通讯机构
摘要:
The escalation of multidrug-resistant bacterial infections, especially infections caused by methicillin-resistant Staphylococcus aureus (MRSA), underscores the urgent need for novel antimicrobial drugs. Here, we synthesized a series of amphiphilic 2-phenyl-1H-phenanthro[9,10-d]imidazole-antimicrobial peptide (AMP) mimic conjugates (III1-30). Among them, compound III13 exhibited excellent antibacterial activity against G+ bacteria and clinical MRSA isolates (MIC = 0.5-2 μg/mL), high membrane selectivity, and low toxicity. Additionally, compared...

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