Amareshwar Vijayalaxmi, Patil S J, Goudgaon N M
Department of Chemistry, Gulbarga University, Gulbarga-585 106, India.
Indian J Pharm Sci. 2010 Nov;72(6):778-81. doi: 10.4103/0250-474X.84593.
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.
合成了一种嘧啶核苷碱基、5-苯硫基-2,4-双苄氧基嘧啶及其类似物，并采用杯碟法和常量肉汤稀释法检测其对白色念珠菌、黑曲霉、黄曲霉和烟曲霉的体外抗真菌活性。在杯碟法中，5-苯硫基-2,4-双苄氧基嘧啶在100和1000μg/ml浓度下与克霉唑相比显示出非常好的抗真菌活性，在常量肉汤稀释法中，它与标准药物氟康唑和伊曲康唑具有相当的活性。5-苯硫基-2,4-双苄氧基嘧啶在10和30mg/kg剂量水平下的体内抗真菌活性是通过使用体外试验中相同的真菌引起小鼠全身感染来进行的。5-苯硫基-2,4-双苄氧基嘧啶和氟康唑的体内研究结果表明，5-苯硫基-2,4-双苄氧基嘧啶在两个剂量水平下的效力与氟康唑相似。
