Introduction
We have reported that some 4-nitrosopyrazoles derivatives displayed in
vitro and in vivo potent antifungal activity at no cytotoxic concentration
and some of these compounds were 4 times more potent than
Amphotericine B and Fluconazole respectively against Cryptococcus
Neoformans and C. Krusei.
We reported also that the absence of NO group or its replacement with
NO2 or NH2 groups gave compounds devoid of antimycotical activity.
Aim of the work
To better understand the mechanism of action and with the aim of
identifying the chemical features responsible for the action, we
synthesized and tested a new class of compounds in which the 4-NO group
was replaced with 4-CN group having, these last, similar steric and
electronic features, but different routes by which may be metabolized in
vivo.
Result
The title compounds tested in vitro for antifungal activity against C.
Neoformans and C. Krusei, displayed an interesting antifungal activity,
increased compared to the analogous 4-NO-pyrazole
