| Autor: |
Ahmed H. Abdelazeem, Alaa M. Alqahtani, Asmaa G. Safi El-Din, Randa Abdou, Ali H. Amin, Hany H. Arab |
| Rok vydání: |
2022 |
| Předmět: |
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| Zdroj: |
Letters in Drug Design & Discovery. 19:925-937 |
| ISSN: |
1570-1808 |
| DOI: |
10.2174/1570180819666220301154851 |
| Popis: |
Background: The search for novel antimicrobial agents effective against the emerging resistant pathogenic microorganisms to the currently used drugs is a substantial need. Herein, a novel series of compounds bearing a benzothiazolotriazole scaffold was synthesized and evaluated as potential antimicrobial agents against a panel of gram +ve, gram -ve bacteria, and fungi species. Methods: The new compounds were synthesized via hybridization between the benzothiazolotriazole scaffold and thiadiazole ring or various substituted aromatic moieties using the tethering technique in drug discovery. Results: The in vitro results revealed that these compounds have significant antifungal activity rather than antibacterial potential due to their high similarity with tricyclazole. Compound 7b bearing bromo-phenyl moiety was the most potent derivative with an MIC value of 8 μg/mL against Candida albicans and Penicillium chrysogenum. Conclusion: Collectively, benzothiazolotriazole-based derivatives are good antifungal leads and should be further actively pursued to expand treatment options for systemic and topical fungal infections. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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