Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Eur J Med Chem. 2017 Jul 28;135:241-259. doi: 10.1016/j.ejmech.2017.04.044. Epub 2017 Apr 21.
The azole antifungal drugs are an important class of chemotherapeutic agents with broad-spectrum of activity against yeasts and filamentous fungi, act in the ergosterol biosynthetic pathway through inhibition of the cytochrome P450-dependent enzyme sterol 14α-demethylase. Azole antifungals have also been repurposed for treatment of tropical protozoan infections including human leishmaniasis. Recent advances in molecular biology and computational chemistry areas have increased our knowledge about sterol biochemical pathway in Leishmania parasites. Based on the importance of sterol biosynthetic pathway in Leishmania parasites, we reviewed all studies reported on azoles for potential antileishmanial therapy along their structural and biological aspects. This review may help medicinal chemists for design of new azole-derived antileishmanial drugs.
唑类抗真菌药物是一类重要的化疗药物，具有广谱抗酵母和丝状真菌的活性，通过抑制细胞色素 P450 依赖性酶固醇 14α-脱甲基酶在麦角固醇生物合成途径中发挥作用。唑类抗真菌药物也被重新用于治疗热带原生动物感染，包括人类利什曼病。分子生物学和计算化学领域的最新进展增加了我们对利什曼原虫固醇生物化学途径的了解。基于固醇生物合成途径在利什曼原虫中的重要性，我们综述了所有关于唑类药物在潜在抗利什曼原虫治疗方面的结构和生物学方面的研究。这篇综述可能有助于药物化学家设计新的唑类衍生的抗利什曼原虫药物。
