琉璃苣毒素 A 的新 3-酰基衍生物：设计、合成和体外抗菌活性。

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2024-11-20 DOI:10.1080/10286020.2024.2429136

Wei-Xian Yang, Wei-Qing Zhang, Mei-Qi Wei, Mei-Hui Duan, Xian-Ji Liu, Chen Yan

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引用次数: 0

摘要

为了发现新型抗菌药物，研究人员通过对琉璃苣毒素 A 进行 A 环修饰，合成了 22 种新型酰化衍生物。评估了这些化合物对粪大肠杆菌、粪肠球菌、MRSA、大肠杆菌、鲍曼不动杆菌和肺炎双球菌的体外抗菌活性。结果表明，化合物 3d 对粪肠球菌、屎肠球菌和 MRSA 的最低抑制浓度为 4 μg/ml。进一步的分子对接显示，化合物 3d 具有更高的结合亲和力。总之，化合物 3d 有潜力发展成为一种抗耐药细菌的新药。

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New 3-acyl derivatives of glaucocalyxin A: designed, synthesis and in vitro antibacterial activities.

To discover novel antimicrobial drug, 22 novel acylated derivatives were synthesized by A-ring modification of glaucocalyxin A. The structures of these derivatives were confirmed by NMR and MS data. In vitro antimicrobial activity of these compounds was evaluated against E. faecium, E. faecalis, MRSA, E. coli, A. baumannii and K. pneumoniae. The results showed compound 3d against E. faecium, E. faecalis and MRSA with a minimum inhibitory concentration of 4 μg/ml. And further molecular docking revealed that compound 3d has a higher binding affinity. In conclusion, compound 3d has the potential to develop into a new drug against drug-resistant bacteria.

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

审稿时长

2.3 months

期刊介绍： The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures. All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.