Nosiheptide analogues as potential antibacterial agents via dehydroalanine region modifications: Semi-synthesis, antimicrobial activity and molecular docking study
文献类型：期刊论文
| 作者 | Fan, Yafei2; Chen, Hangfei3; Mu, Ning2; Wang, Wengui2; Zhu, Kongkai1,4; Ruan, Zhi3; Wang, Shoufeng2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2021-02-01 |
| 卷号 | 31页码:10 |
| 关键词 | Nosiheptide analogues Semi-synthesis Antimicrobial activity Molecular docking |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2020.115970 |
| 通讯作者 | Zhu, Kongkai(bio_zhukk@ujn.edu.cn) ; Ruan, Zhi(r_z@zju.edu.cn) ; Wang, Shoufeng(chm_wangsf@ujn.edu.cn) |
| 英文摘要 | The frequent and inappropriate use of antibiotics aggravate the variation and evolution of multidrug-resistant bacteria, posing a serious threat to public health. Nosiheptide (NOS) has excellent lethality against a variety of Gram-positive bacteria, however the physical and chemical drawbacks hamper its routine application in clinical practice. In this study, by using NOS as the starting material, a total of 15 NOS analogues (2a-4e) were semi-synthesized via its dehydroalanine residue reacting with monosubstituted anilines. In vitro antimicrobial susceptibilities of NOS and its analogues against two methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE) clinical isolates were determined by broth microdilution assay to determine the minimum inhibitory concentration (MIC). Antimicrobial susceptibility testing data shown that most of the NOS analogues had a better antibacterial effect than the parent compound, with compound 3c exhibiting the highest antibacterial activity against VRE (MIC = 0.0078 mg/L) and MRSA (MIC < 0.0039 mg/L). Molecular docking of synthetic compounds was also performed to verify the binding interactions of NOS analogues with the target. Our data indicated that compound 3c possesses stronger and more complex intermolecular force than other analogues, which is consistent with the results of the biological activity evaluation. Overall, this study identified a number of potential antibacterial NOS analogues that could act as potent therapeutic agents for multidrug-resistant bacterial infections. |
| 资助项目 | National Natural Science Foundation of China[31972850] ; Shandong Key Research Program[2019GSF108223] ; State Key Laboratory of Microbial Technology Open Projects Fund[M2020-05] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000616108800004 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/295719]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Zhu, Kongkai; Ruan, Zhi; Wang, Shoufeng |
| 作者单位 | 1.Univ Jinan, Sch Biol Sci & Technol, Jinan 250022, Peoples R China 2.Univ Jinan, Sch Chem & Chem Engn, Shandong Prov Key Lab Fluorine Chem & Chem Mat, Jinan 250022, Peoples R China 3.Zhejiang Univ, Sch Med, Sir Run Run Shaw Hosp, Dept Clin Lab, Hangzhou 310016, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fan, Yafei,Chen, Hangfei,Mu, Ning,et al. Nosiheptide analogues as potential antibacterial agents via dehydroalanine region modifications: Semi-synthesis, antimicrobial activity and molecular docking study[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2021,31:10. |
| APA | Fan, Yafei.,Chen, Hangfei.,Mu, Ning.,Wang, Wengui.,Zhu, Kongkai.,...&Wang, Shoufeng.(2021).Nosiheptide analogues as potential antibacterial agents via dehydroalanine region modifications: Semi-synthesis, antimicrobial activity and molecular docking study.BIOORGANIC & MEDICINAL CHEMISTRY,31,10. |
| MLA | Fan, Yafei,et al."Nosiheptide analogues as potential antibacterial agents via dehydroalanine region modifications: Semi-synthesis, antimicrobial activity and molecular docking study".BIOORGANIC & MEDICINAL CHEMISTRY 31(2021):10. |
入库方式： OAI收割
来源：上海药物研究所
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