Scholarlink

<p>In this study, a series of indole-based derivatives (<b>2a–f</b>) was synthesized, followed by a Mannich base reaction from the starting materials, substituted phenylhydrazine and substituted acetophenone, in glacial acetic acid. All the synthesized derivatives were characterized by <b>IR</b>, <b>NMR</b>, <b>Mass</b> and screened for anticonvulsant activity using the maximal electroshock model. Among all, 2b, 2c and 2e exhibited potent anticonvulsant activity as compared to standard drug phenytoin sodium. In our study, we carried out an in-silico study against GABA receptor, and the AMPA-sensitive glutamate. Docking study revealed that <b>2b, 2c, 2e</b> showed good binding energy against AMPA receptor. Among the six synthesized compounds <b>2b, 2c</b>, and <b>2e</b> were found to possess an optimum to excellent <i>in- silico</i> ADME properties. Our results showed that substituting a 2-phenylindole derivative also increases the therapeutic value of the 2-phenylindole core, which is needed for the discovery of a potent anticonvulsant agent.</p> Graphical abstract

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, In-silico and In-vivo anticonvulsant activity of substituted 2-Phenyl Indole derivatives

  • 期刊论文

  • 发表日期：

    2026年2月2日

查看全文
  • Lateef Khan,
  • Shobha Singh,
  • Divyash Singh,
  • Dharamveer Panjwani,
  • Avinash Chandra Tripathi

摘要

In this study, a series of indole-based derivatives (2a–f) was synthesized, followed by a Mannich base reaction from the starting materials, substituted phenylhydrazine and substituted acetophenone, in glacial acetic acid. All the synthesized derivatives were characterized by IR, NMR, Mass and screened for anticonvulsant activity using the maximal electroshock model. Among all, 2b, 2c and 2e exhibited potent anticonvulsant activity as compared to standard drug phenytoin sodium. In our study, we carried out an in-silico study against GABA receptor, and the AMPA-sensitive glutamate. Docking study revealed that 2b, 2c, 2e showed good binding energy against AMPA receptor. Among the six synthesized compounds 2b, 2c, and 2e were found to possess an optimum to excellent in- silico ADME properties. Our results showed that substituting a 2-phenylindole derivative also increases the therapeutic value of the 2-phenylindole core, which is needed for the discovery of a potent anticonvulsant agent.

Graphical abstract