Antidermatophytic action of new 1-naphthylmethyl and benzo[b]thiophen-7-ylmethyl hydrazones related to inhibitors of squalene epoxidase.
Two series of hydrazonic compounds related to main classes of inhibitors of fungal squalene epoxidase (SE) were designed and prepared on the hypothesis of a pharmacophoric model. The antifungal activity of the new compounds was evaluated in vitro against dermatophytes, moulds and yeasts. Antidermatophytic activity resulted for several hydrazones, particularly for those containing a tett-butylacetylenic group, supporting the hypothesis that the introduction of a hydrazonic function in the model could retain the antimycotic activity.
Auzzas
L
L
Dipartimento Farmaco Chimico Tossicologico, University of Sassari, Italy. anfarm@ssmain.uniss.it
Palomba
M
M
Boatto
G
G
Manconi
P
P
Pau
A
A
Becciu
A
A
Cerri
R
R
Tullio
V
V
Roana
J
J
Carlone
N
N
D003883:Arthrodermataceae / Q000187:drug effects*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D005658:Fungi / Q000187:drug effects; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D010105:Oxygenases / Q000037:antagonists & inhibitors*; D050603:Squalene Monooxygenase; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology
D004791:Enzyme Inhibitors; D006835:Hydrazones; D009281:Naphthalenes; D013876:Thiophenes; D010105:Oxygenases; D050603:Squalene Monooxygenase