Pawar Bhakti, Kanyalkar Meena, Srivastava Sudha
Prin K M Kundnani College of Pharmacy, Cuffe Parade, Mumbai-400005, India.
Biochim Biophys Acta. 2010 Nov;1798(11):2067-75. doi: 10.1016/j.bbamem.2010.06.020. Epub 2010 Jun 30.
Resistance to currently available antifungal drugs necessitates development of new drugs using rapid, robust and automated methods to test a large number of newly synthesized drugs in less time. We have compared the effect of ketoconazole, fluconazole and its synthesized analogues on Candida albicans ATCC 10231. A metabolic profile of C.albicans ATCC 10231 in presence of drugs has been compared using (1)H NMR. Signals from metabolites have been monitored with time. MIC determined using conventional methods has been compared with Metabolic End Point (MEP) obtained from NMR spectroscopy. Results indicate that the activity of the fluconazole derivatives is in the order fluconazole p-methoxybenzoate>fluconazole=fluconazole benzoate>fluconazole toluate>fluconazole p-nitrobenzoate.
对目前可用抗真菌药物产生的耐药性使得有必要开发新药物，这需要采用快速、可靠且自动化的方法，以便在更短时间内测试大量新合成的药物。我们比较了酮康唑、氟康唑及其合成类似物对白色念珠菌ATCC 10231的作用。使用核磁共振氢谱（¹H NMR）比较了白色念珠菌ATCC 10231在药物存在下的代谢谱。随着时间的推移监测代谢物的信号。将使用传统方法测定的最低抑菌浓度（MIC）与从核磁共振光谱获得的代谢终点（MEP）进行了比较。结果表明，氟康唑衍生物的活性顺序为：对甲氧基苯甲酸氟康唑＞氟康唑=苯甲酸氟康唑＞甲苯酸氟康唑＞对硝基苯甲酸氟康唑。
