1. 2-(benzylideneamino)phenol: a promising hydroxyaldimine with potent activity against dermatophytoses.
- Author
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Gasparto AK, Baltazar LM, Gouveia LF, da Silva CM, Byrro RM, Rachid MA, Cunha Júnior Ada S, de Resende-Stoianoff MA, de Fátima A, and Santos DA
- Subjects
- Animals, Antifungal Agents chemical synthesis, Antifungal Agents chemistry, Female, Humans, Male, Mice, Mice, Inbred BALB C, Microbial Sensitivity Tests, Phenol chemistry, Tinea drug therapy, Trichophyton genetics, Trichophyton isolation & purification, Trichophyton physiology, Antifungal Agents pharmacology, Phenol pharmacology, Tinea microbiology, Trichophyton drug effects
- Abstract
Infections caused by dermatophytes, mainly Trichophyton rubrum,are often vulnerable to relapses upon cessation of antifungal therapy, reinforcing the need of new antifungals. Aldimines have potential biological activities, but there are few reports on their antifungal profile. The aim of this study was to evaluate the antifungal activity of 2-(benzylideneamino)phenol (3A3) and 4-(benzylideneamino)phenol (3A4) against dermatophytes. We determined the minimum inhibitory concentration, minimum fungicidal concentration, time-kill curves and fractional inhibitory concentration of the combination of 3A3, 3A4 and itraconazole against a set of isolates of T. rubrum and T. interdigitale. 3A3 was tested in a murine model of dermatophytoses caused by T. rubrum, and the effect on phagocytosis was assessed. The MIC values ranged from 8 to 32 μg/mL for 3A3 and from 64 to 256 μg/mL for 3A4. The interaction between 3A3 and 3A4 with itraconazole proved to be synergistic and indifferent, respectively. 3A3 was as efficient as itraconazole in reducing the fungal burden on the skin of mice, being this effect associated with the influx of neutrophil and macrophage. Also, 3A3 was able to increase the internalization of conidia by macrophages. Altogether, our data encourage future clinical studies with 3A3 to treat dermatophytoses.
- Published
- 2015
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