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Synthesis, In Vitro and In Vivo antifungal activity of 5-phenylthio-2,4-bisbenzyloxypyrimidine: A novel nucleobase

Author(s): Vijayalaxmi Amareshwar1, SJ Patil2, NM Goudgaon1
1Department of Chemistry, Gulbarga University, Gulbarga-585 106, India 2Department of Zoology, Gulbarga University, Gulbarga-585 106, India

Correspondence Address:
Vijayalaxmi Amareshwar Department of Chemistry, Gulbarga University, Gulbarga-585 106 India E-mail: [email protected]

A pyrimidne nucleobase, 5-phenylthio-2,4-bisbenzyloxypyrimidine and its analogs were synthesized and scanned for in vitro antifungal activity using cup-plate and macrobroth dilution method against Candida albicans, Aspergillus niger, Aspergillus flavus and Aspergllus fumigatus. In the cup-plate method, 5-phenylthio-2,4-bisbenzyloxypyrimidine showed very good antifungal activity compared to clotrimazole at the concentrations of 100 and 1000 μg/ml and in the macrobroth dilution method, it showed comparable activity with respect to standard drugs fluconazole and itraconaole. In vivo antifungal activity of 5-phenylthio-2,4-bisbenzyloxypyrimidine at the dose levels of 10 and 30 mg/kg was carried by causing systemic infection of mice using the same fungi used in in vitro testing. The results from in vivo studies with 5-phenylthio-2,4-bisbenzyloxypyrimidine and fluconazole indicated that 5-phenylthio-2,4-bisbenzyloxypyrimidine had similar potency as fluconazole at both dose levels.

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