Scholarlink

Abstract <p>Thiazole hybrid frameworks constitute a promising class of compounds in the field of drug discovery, attracting significant attention due to their wide range of applications. In this study, we designed novel coumarin-based thiazole hybrids. 3-(1-{2-[4-(4-R-phenyl)-1,3-thiazol-2-yl]hydrazinylidene}ethyl)-2<i>H</i>-chromen-2-one derivatives <b>4a</b>–<b>4h</b> bearing a methoxy group at the 8-position or a bromine atom at the 6-position of the coumarin moiety, through a one-pot three-component reaction. The synthesized compounds were characterized using spectroscopic techniques and subjected to DFT (Density Functional Theory) studies, including HOMO–LUMO analysis and MEP (Molecular Electrostatic Potential) mapping. Antimicrobial evaluation of the newly synthesized derivatives revealed that compounds <b>4d</b> and <b>4h</b> exhibited excellent antibacterial activity, with a significant zone of inhibition against <i>Staphylococcus aureus</i>. The results of antifungal assay showed that compound <b>4c</b> was potent against <i>Aspergillus niger</i>, while compounds <b>4a</b> and <b>4e</b> exhibited potent antifungal activity against <i>Penicillium chrysogenum</i>.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Synthesis, Characterization, Computational Study, and Biological Activity of Novel Coumarin–Thiazole Hybrids

  • 期刊论文

  • 发表日期：

    2026年2月1日

查看全文
  • P. Sudeep,
  • S. A. Bhat,
  • A. K. Kariyappa

摘要

Abstract

Thiazole hybrid frameworks constitute a promising class of compounds in the field of drug discovery, attracting significant attention due to their wide range of applications. In this study, we designed novel coumarin-based thiazole hybrids. 3-(1-{2-[4-(4-R-phenyl)-1,3-thiazol-2-yl]hydrazinylidene}ethyl)-2H-chromen-2-one derivatives 4a–4h bearing a methoxy group at the 8-position or a bromine atom at the 6-position of the coumarin moiety, through a one-pot three-component reaction. The synthesized compounds were characterized using spectroscopic techniques and subjected to DFT (Density Functional Theory) studies, including HOMO–LUMO analysis and MEP (Molecular Electrostatic Potential) mapping. Antimicrobial evaluation of the newly synthesized derivatives revealed that compounds 4d and 4h exhibited excellent antibacterial activity, with a significant zone of inhibition against Staphylococcus aureus. The results of antifungal assay showed that compound 4c was potent against Aspergillus niger, while compounds 4a and 4e exhibited potent antifungal activity against Penicillium chrysogenum.