Synthesis and biological evaluation of novel aminoguanidine derivatives as potential antibacterial agents.

IF 3.8 2区综合性期刊 Q1 MULTIDISCIPLINARY SCIENCES

Scientific Reports Pub Date : 2024-11-06 DOI:10.1038/s41598-024-77668-0

Xueqian Bai, Jinghan Wang, Feitong Jiao, Hongmei Zhang, Tianyi Zhang

引用次数: 0

Abstract

In an effort to identify novel antibacterial agents, we presented two series of aminoguanidine derivatives that were designed by incorporating 1,2,4-triazol moieties. All compounds exhibited strong in vitro antibacterial activity against a variety of testing strains. Compound 5f was identified as a potent antibacterial agent with a minimum inhibitory concentration (MIC) of 2-8 µg/mL against S. aureus, E. coli, S. epidermidis, B. subtilis, C. albicans, multi-drug resistant Staphylococcus aureus and multi-drug resistant Escherichia coli and low toxicity (Hela > 100 µM). Membrane permeability and transmission electron microscopy (TEM) image studies demonstrated that compound 5f permeabilized bacterial membranes, resulting in irregular cell morphology and the rapid death of bacteria. The results of the present study suggested that aminoguanidine derivatives with 1,2,4-triazol moieties were the intriguing scaffolds for the development of bactericidal agents.

查看原文本刊更多论文

作为潜在抗菌剂的新型氨基胍衍生物的合成和生物学评价。

为了寻找新型抗菌剂，我们提出了两个系列的氨基胍衍生物，这些衍生物是通过加入 1,2,4- 三唑分子设计而成的。所有化合物对多种试验菌株都表现出很强的体外抗菌活性。化合物 5f 被确定为一种强效抗菌剂，对金黄色葡萄球菌、大肠杆菌、表皮葡萄球菌、枯草杆菌、白僵菌、耐多药金黄色葡萄球菌和耐多药大肠杆菌的最低抑菌浓度（MIC）为 2-8 µg/mL，且毒性低（Hela > 100 µM）。膜渗透性和透射电子显微镜（TEM）图像研究表明，化合物 5f 可使细菌膜渗透，导致细胞形态不规则和细菌快速死亡。本研究的结果表明，具有 1,2,4-三唑分子的氨基胍衍生物是开发杀菌剂的有趣支架。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Scientific Reports Natural Science Disciplines-

CiteScore

7.50

自引率

4.30%

发文量

19567

审稿时长

3.9 months

期刊介绍： We publish original research from all areas of the natural sciences, psychology, medicine and engineering. You can learn more about what we publish by browsing our specific scientific subject areas below or explore Scientific Reports by browsing all articles and collections. Scientific Reports has a 2-year impact factor: 4.380 (2021), and is the 6th most-cited journal in the world, with more than 540,000 citations in 2020 (Clarivate Analytics, 2021). •Engineering Engineering covers all aspects of engineering, technology, and applied science. It plays a crucial role in the development of technologies to address some of the world''s biggest challenges, helping to save lives and improve the way we live. •Physical sciences Physical sciences are those academic disciplines that aim to uncover the underlying laws of nature — often written in the language of mathematics. It is a collective term for areas of study including astronomy, chemistry, materials science and physics. •Earth and environmental sciences Earth and environmental sciences cover all aspects of Earth and planetary science and broadly encompass solid Earth processes, surface and atmospheric dynamics, Earth system history, climate and climate change, marine and freshwater systems, and ecology. It also considers the interactions between humans and these systems. •Biological sciences Biological sciences encompass all the divisions of natural sciences examining various aspects of vital processes. The concept includes anatomy, physiology, cell biology, biochemistry and biophysics, and covers all organisms from microorganisms, animals to plants. •Health sciences The health sciences study health, disease and healthcare. This field of study aims to develop knowledge, interventions and technology for use in healthcare to improve the treatment of patients.