ABSTRACT
Fluconazole (“Diflucan”), 2,4-difluoro-α,α1-bis (1H-1,2,4-triazol-1-ylmethyl) benzyl alcohol, was the first of class of synthetic bis-triazole antifungal agent. It has the chemical formula C13H12F2N6O and a molecular weight of 306.3. The chemical structure is shown in Figure 153.1. The primary mode of action of fluconazole is selective inhibition of fungal cytochrome P450-dependent C14-α sterol demethylase which is involved in the biosynthesis of fungal ergosterol. This leads to loss of normal sterols and in turn, accumulation of 14-αmethyl ergosterol precursors in the fungal plasma membrane, ultimately resulting in fungal growth arrest (see later under 3, Mechanism of drug action). It was licensed in the United States by the Food and Drug Adminsitration (FDA) in January 1990 to treat candidal and cryptococcal infections. Chemical structure of fluconazole. https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig153_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/>
