Identification of Coumarin-Chalcone and Coumarin-Pyrazoline Derivatives as Novel Anti- Toxoplasma gondii Agents.
| Autor: | Ebaid MS; Department of Chemistry, College of Science, Northern Border University, Arar, Saudi Arabia.; Chemistry of Natural Compounds Department, Pharmaceutical and Drug Industries Research Institute, National Research Center, Dokki, Cairo, Egypt., Chyb M; Department of Molecular Microbiology, Faculty of Biology and Environmental Protection, University of Lodz, Łódź, Poland.; Bio-Med-Chem Doctoral School of the University of Lodz and Lodz Institutes of the Polish Academy of Sciences, Łódź, Poland., Furlan V; Faculty of Chemistry and Chemical Engineering, University of Maribor, Maribor, Slovenia., Ibrahim HAA; Pediatric Department, Faculty of Medicine, Cairo University, Cairo, Egypt., Bren U; Faculty of Chemistry and Chemical Engineering, University of Maribor, Maribor, Slovenia.; Faculty of Mathematics, Natural Sciences and Information Technologies, University of Primorska, Glagoljaška 8, Slovenia.; Institute of Environmental Protection and Sensors, Beloruska Ulica 7, Maribor, Slovenia., Gatkowska J; Department of Molecular Microbiology, Faculty of Biology and Environmental Protection, University of Lodz, Łódź, Poland., Dziadek J; Laboratory of Genetics and Physiology of Mycobacterium, Institute of Medical Biology of the Polish Academy of Sciences, Łódź, Poland., Eldehna WM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt.; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Pharos University in Alexandria, Alexandria, Egypt., Sabt A; Chemistry of Natural Compounds Department, Pharmaceutical and Drug Industries Research Institute, National Research Center, Dokki, Cairo, Egypt. |
|---|---|
| Jazyk: | angličtina |
| Zdroj: | Drug design, development and therapy [Drug Des Devel Ther] 2024 Dec 04; Vol. 18, pp. 5599-5614. Date of Electronic Publication: 2024 Dec 04 (Print Publication: 2024). |
| DOI: | 10.2147/DDDT.S495089 |
| Abstrakt: | Introduction: Toxoplasmosis, a zoonotic infection caused by the apicomplexan parasite Toxoplasma gondii , affects a significant portion of the global human population. This condition, particularly dangerous for pregnant women and immunocompromised individuals, currently lacks effective treatment options. Methods: Eighteen coumarin-based derivatives were synthesized, comprising coumarin-chalcone hybrids (5a-i) and coumarin-pyrazoline hybrids (6a-i). Cytotoxicity was evaluated using L929 mouse fibroblasts and Hs27 human fibroblasts. Anti- T. gondii activity was assessed, and molecular docking studies were performed to predict binding modes with TgCDPK1. Results: Pyrazoline hybrids (6a-i) showed lower toxicity than chalcone-bearing coumarins (5a-i), with CC Conclusion: This study highlights the potential of coumarin-based hybrids as anti- T. gondii agents. The findings should contribute to the growing arsenal of small molecules against T. gondii and underscore the value of molecular hybridization in drug design. Further studies to elucidate these compounds' mechanism of action and in vivo efficacy are warranted to fully realize their potential as anti-parasitic agents. Competing Interests: Authors declare no conflict of interest. The authors alone are responsible for the content and writing of the paper. (© 2024 Ebaid et al.) |
| Databáze: | MEDLINE |
| Externí odkaz: |
|