Synthesis and antibacterial evaluation of novel psoralen derivatives against methicillin-resistant Staphylococcus aureus (MRSA)

被引：1

作者：

Yang, Hang ^{[1
,2
]}

Yao, Zheng ^{[1
]}

Yang, Keli ^{[1
,2
]}

Wang, Chuanhao ^{[3
,4
]}

Li, Mochenxuan ^{[2
,4
]}

Zhang, Yanming ^{[2
]}

Yan, Jianyu ^{[2
]}

Lv, Rongxue ^{[1
]}

Wang, Yongchuang ^{[1
,2
]}

Huang, Anhua ^{[1
]}

Zhang, Daozuan ^{[1
]}

Li, Wei ^{[4
]}

Wu, Yuelin ^{[1
]}

Miao, Zhenyuan ^{[2
]}

机构：

[1] Shanghai Inst Technol, Sch Chem & Environm Engn, Haiquan Rd 100, Shanghai 201418, Peoples R China

[2] Second Mil Med Univ, Sch Pharm, 325 Guohe Rd, Shanghai 200433, Peoples R China

[3] Nanjing Univ Sci & Technol, Sch Chem Engn, 200 XiaoLingWei Rd, Nanjing 210094, Peoples R China

[4] East China Univ Sci & Technol, Sch Pharm, 130 Meilong Rd, Shanghai 200237, Peoples R China

来源：

CHEMISTRY & BIODIVERSITY | 2024年 / 21卷 / 08期

基金：

中国国家自然科学基金;

关键词：

psoralen; MRSA; antibacterial activity; scaffold hopping; INHIBITORS;

D O I：

10.1002/cbdv.202302048

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Today, the bacterial infections caused by multidrug-resistant pathogens seriously threaten human health. Thereby, there is an urgent need to discover antibacterial drugs with novel mechanism. Here, novel psoralen derivatives had been designed and synthesized by a scaffold hopping strategy. Among these targeted twenty-five compounds, compound ZM631 showed the best antibacterial activity against methicillin-resistant S. aureus (MRSA) with the low MIC of 1 mu g/mL which is 2-fold more active than that of the positive drug gepotidacin. Molecular docking study revealed that compound ZM631 fitted well in the active pockets of bacterial S. aureus DNA gyrase and formed a key hydrogen bond binding with the residue ASP-1083. These findings demonstrated that the psoralen scaffold could serve as an antibacterial lead compound for further drug development against multidrug-resistant bacterial infections.

引用

页数：10

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