An overview of azoles targeting sterol 14α-demethylase for antileishmanial therapy

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 14 alpha-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. (C) 2017 Elsevier Masson SAS. All rights reserved.