Scholarlink

<p>New formyl indole derivatives based on thiobarbituric acid were designed for targeting parasitological applications. The new compounds (5-((1<i>H</i>-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1<i>H</i>,5<i>H</i>)-dione (<b>3a</b>), and 5-((1-benzyl-1<i>H</i>-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1<i>H</i>,5<i>H</i>)-dione (<b>3b</b>) were synthesized as thioxodihydropyrimidine derivatives <i>via</i> aldol condensation reaction. The structures of the synthesized compounds were confirmed based on their spectral data <i>via</i> FT-IR, <sup>1</sup>H and <sup>13</sup>C NMR spectral characterization. In addition, the structure of <b>3a</b> is confirmed using X-ray crystallography. The synthesized compounds were prepared in nm scale <i>via</i> chitosan as a matrix, and their size was measured <i>via</i> scanning electronic microscope. Interestingly, the newly synthesized nano formulations show higher positive zeta potential (mV) values <b>+ 29.6</b> and <b>+ 26.1</b> for compounds <b>NP-3a</b>, and <b>NP-3b</b>; respectively. These compounds were tested for their parasitological activity. The results revealed that <b>3b</b> had a great activity against cryptosporidium infection. Moreover, the nano formulation of compound <b>3b</b> showed a significant reduction percent of oocyst count of cryptosporidium infected mice representing 66%. Furthermore, these compounds were screened by in-vitro hemolytic activity assay (IC<sub>50</sub>) values (cytotoxicity on RBCs) to assess their cytotoxic potentials and safety profiles.</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

New formyl indole derivatives based on thiobarbituric acid and their nano-formulations; synthesis, characterization, parasitology and histopathology investigations

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年1月2日

查看全文
  • Walaa Ali Abdelhalim,
  • Ahmed R. Rabee,
  • Saied M. Soliman,
  • Mohamed Hagar,
  • Esraa A. Moneer,
  • Basant A. Bakr,
  • Assem Barakat,
  • Matti Haukka,
  • Hanaa A. Rasheed

摘要

New formyl indole derivatives based on thiobarbituric acid were designed for targeting parasitological applications. The new compounds (5-((1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (3a), and 5-((1-benzyl-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (3b) were synthesized as thioxodihydropyrimidine derivatives via aldol condensation reaction. The structures of the synthesized compounds were confirmed based on their spectral data via FT-IR, 1H and 13C NMR spectral characterization. In addition, the structure of 3a is confirmed using X-ray crystallography. The synthesized compounds were prepared in nm scale via chitosan as a matrix, and their size was measured via scanning electronic microscope. Interestingly, the newly synthesized nano formulations show higher positive zeta potential (mV) values + 29.6 and + 26.1 for compounds NP-3a, and NP-3b; respectively. These compounds were tested for their parasitological activity. The results revealed that 3b had a great activity against cryptosporidium infection. Moreover, the nano formulation of compound 3b showed a significant reduction percent of oocyst count of cryptosporidium infected mice representing 66%. Furthermore, these compounds were screened by in-vitro hemolytic activity assay (IC50) values (cytotoxicity on RBCs) to assess their cytotoxic potentials and safety profiles.