Details

Autor(en) / Beteiligte

• Emami, Saeed
• Tavangar, Pegah
• Keighobadi, Masoud

Titel

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

Ist Teil von

• European journal of medicinal chemistry, 2017-07, Vol.135, p.241-259

Ort / Verlag

France: Elsevier Masson SAS

Erscheinungsjahr

2017

Quelle

MEDLINE

Beschreibungen/Notizen

• 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. This review describes the current aspects of sterol biochemical pathway in Leishmania parasites and the importance of azoles for targeting of sterol 14α-demethylase in the field of antileishmanial therapy. [Display omitted] •The importance of sterol biochemical pathway in Leishmania parasites was described.•In sterol pathway, 14α-demethylase is a distinct target for antileishmanial therapy.•Azole antifungals are well-known inhibitors of sterol 14α-demethylase.•Azole antifungals have been repurposed for treatment of human Leishmaniasis.•Structural refinement is necessity for design of potent azole antileishmanials.