Salvato in:
| Autori principali: | , , |
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| Natura: | Recurso digital |
| Lingua: | inglese |
| Pubblicazione: |
Zenodo
2023
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| Accesso online: | https://doi.org/10.1155/2023/8992853 |
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Sommario:
- <p>Purpose. To synthesize new isoindole-1,3(2H)-dione derivatives by molecular hybridization of gabapentin and pregabalin with<br>phthalic anhydride derivatives and to evaluate their biological activity as promising antioxidant, antimicrobial, and anticancer<br>agents. Method. Molecular hybridization was successfully achieved by two procedures; synthesized compounds were characterized<br>using analytical and spectral methods. ,e free radical scavenging properties of synthesized compounds were evaluated using the<br>DPPH method. ,e antibacterial activity of synthesized compounds and parent compounds was evaluated against two microbial<br>Gram-positive and Gram-negative strains by the well di<usion method. Furthermore, we have studied the e<ect of compounds on<br>proliferation, cell cycle, and cell death in two human cancer cell lines (Caco-2 and HCT-116). Results. Compounds 1, 3, and 4<br>exhibited a good free radical scavenging e<ect, and compound 3 is the most e<ective with IC50 value of 2.525 *mol/mL. All<br>compounds showed antibacterial activity against Escherichia coli and Staphylococcus aureus related to concentration, while parent<br>drugs did not exhibit any antibacterial e<ect. Compounds 1 and 2 showed a good zone of inhibition against E. coli at micromolar<br>concentrations, and they are more e<ective than Gentamicin Sulfate. Treatment with the studied compounds suppresses<br>proliferation, arrests progress throughout the cell cycle, and induces apoptosis in Caco-2 and HCT-116 cancer cells. Compound 2<br>is highly e<ective against Caco-2 cells and more e<ective than thalidomide, with IC50 value less than 1 *mol/L. Conclusion. Our<br>results showed that molecular hybridization of gabapentin and pregabalin in the isoindole-1,3(2H)-dione moiety results in<br>promising anticancer and antimicrobial molecules. Results of this preliminary study show that halogenation of the isoindole-<br>1,3(2H)-dione moiety improves antimicrobial and anticancer activity and that tetra-brominated derivatives are comparable to or<br>more e<ective than related tetra-chlorinated derivatives.<br>1. Introduction<br>Research for new, safe, and e<ective drugs has been a continuous<br>need over the years, especially since there are still<br>challenging diseases with no su@cient treatments, such as<br>cancer, neurodegenerative diseases, autoimmune diseases,<br>and infectious diseases related to resistant microorganisms.<br>,erapeutic choices for complex, heterogeneous diseases<br>can be</p>