Journal
FUTURE MEDICINAL CHEMISTRY
Volume 11, Issue 20, Pages 2663-2686Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0014
Keywords
Aspergillus; GBB reaction; imidazole; lanosterol 14 alpha-demethylase; nucleosides
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Funding
- Guru Gobind Sing Indraprastha University, New Delhi, India
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Aim: The global burden of fungal infections has transitioned from a case-specific observation to a major cause of high human mortality. Therefore, novel compounds with innovative methodologies need to be synthesized and evaluated for their antifungal potential to keep pace with the current clinical demands. Results: An efficient synthetic pathway was developed for the synthesis of 21 synthetic novel nucleosides. Two compounds had significant antifungal effect on Aspergillus fumigatus 3007, which was comparable to fluconazole. The experimental data (confocal microscopy, ultrahigh-performance liquid chromatography and flow cytometry) demonstrated the inhibition of fungal lanosterol 14 alpha-demethylase. Conclusion: Owing to the therapeutic relevance of the synthesized nucleosides and simplicity of the procedure, the method may find its potential application for synthesis of antifungal agents.
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