A1 Journal article (refereed)
New formyl indole derivatives based on thiobarbituric acid and their nano-formulations : synthesis, characterization, parasitology and histopathology investigations (2025)
Abdelhalim, W. A., Rabee, A. R., Soliman, S. M., Hagar, M., Moneer, E. A., Bakr, B. A., Barakat, A., Haukka, M., & Rasheed, H. A. (2025). New formyl indole derivatives based on thiobarbituric acid and their nano-formulations : synthesis, characterization, parasitology and histopathology investigations. Scientific Reports, 15, Article 299. https://doi.org/10.1038/s41598-024-81683-6
JYU authors or editors
Publication details
All authors or editors: Abdelhalim, Walaa Ali; Rabee, Ahmed R.; Soliman, Saied M.; Hagar, Mohamed; Moneer, Esraa A.; Bakr, Basant A.; Barakat, Assem; Haukka, Matti; Rasheed, Hanaa A.
Journal or series: Scientific Reports
eISSN: 2045-2322
Publication year: 2025
Publication date: 02/01/2025
Volume: 15
Article number: 299
Publisher: Springer Nature
Publication country: United Kingdom
Publication language: English
DOI: https://doi.org/10.1038/s41598-024-81683-6
Publication open access: Openly available
Publication channel open access: Open Access channel
Publication is parallel published (JYX): https://jyx.jyu.fi/handle/123456789/99323
Abstract
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.
Keywords: parasitology; nanostructures; histology; electron microscopy; chemical synthesis; inorganic chemistry
Free keywords: thiobarbituric acid; aldol condensation; nano formulation; parasitology; histopathology investigation
Contributing organizations
Ministry reporting: Yes
VIRTA submission year: 2025
Preliminary JUFO rating: 1