Scholarlink

<p>In this work, 1-phenyl-β-carboline-3-carboxamide-1,2,3-triazole-<i>N</i>-phenylacetamide skeleton as a novel scaffold was designed based on hybridization of moieties that were found in the potent α-glucosidase inhibitors. Fourteen derivatives <b>14a-n</b> of this scaffold were synthesized by the efficient chemical reactions. In vitro anti-α-glucosidase assay demonstrated that all the new fourteen derivatives with IC<sub>50</sub> values ranging from 64.0 to 661.4 µM were more potent than positive control acarbose with IC<sub>50</sub> value of 750.0 and in vitro kinetic study revealed that the most potent compound among them, compound <b>14b</b>, was an uncompetitive α-glucosidase inhibitor. Moreover, determination of the circular dichroism (CD) spectra demonstrated that compound <b>14b</b> altered the secondary structure of α-glucosidase. Prediction of the pharmacokinetics and toxicity of the most potent compound <b>14b</b> showed that our new compound had good toxicity profile as an oral drug candidate. Based on these findings, compound <b>14b</b> can be considered as a promising candidate for the development of a new α-glucosidase inhibitor.</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

1-Phenyl-β-carboline-3-carboxamide-1,2,3-triazole-N-phenylacetamide hybrids as new α-glucosidase inhibitors

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年5月20日

查看全文
  • Elham Safaie,
  • Mohammad Hosein Sayahi,
  • Navid Dastyafteh,
  • Mohammad Halimi,
  • Milad Noori,
  • Maryam Mohammadi-Khanaposhtani,
  • Afsaneh Zonouzi,
  • Roghieh Mirzazadeh,
  • Azadeh Tajmir-Riahi,
  • Somayeh Mojtabavi,
  • Mohammad Ali Faramarzi,
  • Bagher Larijani,
  • Mehdi Asadi,
  • Mohammad Mahdavi

摘要

In this work, 1-phenyl-β-carboline-3-carboxamide-1,2,3-triazole-N-phenylacetamide skeleton as a novel scaffold was designed based on hybridization of moieties that were found in the potent α-glucosidase inhibitors. Fourteen derivatives 14a-n of this scaffold were synthesized by the efficient chemical reactions. In vitro anti-α-glucosidase assay demonstrated that all the new fourteen derivatives with IC50 values ranging from 64.0 to 661.4 µM were more potent than positive control acarbose with IC50 value of 750.0 and in vitro kinetic study revealed that the most potent compound among them, compound 14b, was an uncompetitive α-glucosidase inhibitor. Moreover, determination of the circular dichroism (CD) spectra demonstrated that compound 14b altered the secondary structure of α-glucosidase. Prediction of the pharmacokinetics and toxicity of the most potent compound 14b showed that our new compound had good toxicity profile as an oral drug candidate. Based on these findings, compound 14b can be considered as a promising candidate for the development of a new α-glucosidase inhibitor.