Synthesis, biological evaluation, pharmacological profiling, and molecular docking studies of 4-Aminocoumarin based phenyliodonium derivatives as potent therapeutic agents

以4-氨基香豆素为基础的苯碘鎓衍生物为有效治疗剂的合成、生物学评价、药理学分析和分子对接研究

阅读:1

Abstract

4-Aminocoumarins are significant in organic synthesis as key building blocks for various heterocyclic structures with pharmacological importance. This study focuses on synthesizing phenyliodonium derivatives of 4-aminocoumarins (T1-T6) and evaluating their broad-spectrum biological properties, including antibacterial, antifungal, antiviral, antioxidant, cytotoxicity, and wound-healing properties. The compounds synthesized were structurally confirmed through UV-Vis, GC-MS, (1)H-NMR, (13)C-NMR, FT-IR, melting point, and CHNS analysis. The in vitro antibacterial and antifungal activities of these compounds were assessed against eight bacterial strains and five plant fungal pathogens. The antiviral property was evaluated by measuring the reduction in cytopathic effects of Dengue virus type-2 in BHK-21 cells. Cytotoxicity testing on human epidermal keratinocyte cells using the MTT assay at concentrations ranging from 1 to 100 µg/mL revealed that none of the compounds exhibited significant cytotoxic effects. Additionally, ADME/Toxicity, molecular docking, antioxidant, and wound-healing studies were examined, further supporting the therapeutic potential of these compounds. Most of the synthesized phenyliodonium derivatives demonstrated broad-spectrum antibacterial and antifungal activities. Among them, Compound T6 exhibited the most potent antimicrobial activity, as indicated by its MIC₉₀ and MBC values, demonstrating superior efficacy compared to ciprofloxacin. The antiviral test against Dengue virus type-2 showed minimal effects with a cytopathic effect reduction of 10-13% at non-toxic concentrations. These compounds exhibited broad-spectrum antimicrobial activity coupled with minimal cytotoxicity, highlighting their potential as promising candidates for developing novel therapeutic agents.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。