In vitro antifungal evaluation and studies on the mode of action of xanthoxyline derivatives.
This study describes the fungistatic effect of xanthoxyline (CAS 90-24-4) and its derivatives against a panel of yeasts, filamentous fungi and dermatophytes, by using the agar dilution method. Results indicated that simple structural modifications led to more potent derivatives, especially in relation with dermatophytes. The most active compound tested (10), which is a benzenesulphonyl derivative, was 12-fold more potent than xanthoxyline itself against Trichophyton rubrum. The evaluation of the mode of action with the whole cell Neurospora crassa assay, suggested that some selected compounds may be acting by the inhibition of fungal cell-wall polymers synthesis or assembly.
Pinheiro
T R
TR
Departamento de Quimica, Universidade Federal de Santa Catarina (UFSC), Florianópolis, Brazil.
Yunes
R A
RA
López
S N
SN
Santecchia
C B
CB
Zacchino
S A
SA
Cechinel Filho
V
V
D000098:Acetophenones / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003883:Arthrodermataceae / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005658:Fungi / Q000187:drug effects*; D007654:Ketoconazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009492:Neurospora crassa / Q000187:drug effects / Q000648:ultrastructure; D014249:Trichophyton / Q000187:drug effects; D015003:Yeasts / Q000187:drug effects
D000098:Acetophenones; D000935:Antifungal Agents; D007654:Ketoconazole; C064382:xanthoxyline