063–1 mg/mL showed higher activity than fluconazole against fluconazole-susceptible isolates; significantly, compounds 7b and 7e were also active against
5-16
This drug is an azole antifungal, in the same drug family as [ketoconazole] and [itraconazole]
Azoles block the synthesis of ergosterol, an important component of the fungal cell membrane
Exceptions: Dyphylline
The program began in 1978, and azole derivatives were considered fluconazole derivatives can be foun d in the literature [16]
Volkova * and German L
Two classes of fluconazole derivatives, (a) carboxylic acid esters and (b) fatty alcohol and carbohydrate phosphate esters, were synthesized and evaluated in vitro against Cryptococcus neoformans, Candida albicans, and Aspergillus niger
did not show any sensitivity to any of the compounds
aeruginosa) using ampicillin as reference standard, and these derivatives were also investigated for antifungal activity against C
(Figure 1; Zonios and Bennett, 2008)
The compounds were designed on the basis of the structure of fluconazole and molecular modeling of the active site of the cytochrome P450 14α-demethy
The earlier imidazole derivatives (such as miconazole, econazole, and ketoconazole) Fluconazole and itraconazole are safer alternatives, although the use of itraconazole in patients with significant liver disease is undesirable
cerevisiae mutant strain that overexpresses Pdr5p was used in the assays