The antifungal activity of eight pyrazolo[3,4-c]isothiazole derivatives was evaluated on five 21 dermatophytes: three are anthropophilic species, i.e. Epidermophyton floccosum, Trichophyton 22 rubrum and Trichophyton tonsurans, and two are geophilic species, Microsporum gypseum and 23 Nannizia cajetani. The new compounds proved to be unlikely effective in inhibiting the growth of 24 the different strains. In general the fungi parasitic on man were more sensitive than the geophilic25 species. This fact can be positive for a possible practical-therapeutic utilization of these class of 26 compounds. To verify their possible use against fungi of medical interest, the most interesting 27 substance at low doses, 6-(4-chlorophenyl)-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine, was 28 chosen to perform in vitro genotoxicity tests using: Salmonella/microsome test (SAL), Sister 29 Chromatid Excange test (SCE), Cytokinesis-Blocked Micronucleus test (CBMN) and its 30 improvement (Ara-C/CBMN). The compound showed no mutagenic activity at low doses, whereas 31 at the highest dose (100 μg/mL) it causes a generalized cytotoxic effect. The high growth inhibition32 exerted on fungi at the lowest dose and the concomitant lack of genotoxicity, at least until the dose 33 of 50 μg/mL, might suggest the compound as a safe candidate as antidermatophytic substance.

Antidermatophytic activity of pyrazolo[3,4-c]isothiazoles: a preliminary approach on 4-chlorophenyl derivative for evaluation of mutagenic and clastogenic effects on bacteria and human chromosomes in vitro / D., Rossi; D., Mares; Romagnoli, Carlo; Andreotti, Elisa; S., Manfredini; C. B., Vicentini. - In: DRUG AND CHEMICAL TOXICOLOGY. - ISSN 0148-0545. - STAMPA. - 34:3(2011), pp. 324-331. [10.3109/01480545.2010.536772]

Antidermatophytic activity of pyrazolo[3,4-c]isothiazoles: a preliminary approach on 4-chlorophenyl derivative for evaluation of mutagenic and clastogenic effects on bacteria and human chromosomes in vitro

ROMAGNOLI, Carlo;ANDREOTTI, Elisa;
2011

Abstract

The antifungal activity of eight pyrazolo[3,4-c]isothiazole derivatives was evaluated on five 21 dermatophytes: three are anthropophilic species, i.e. Epidermophyton floccosum, Trichophyton 22 rubrum and Trichophyton tonsurans, and two are geophilic species, Microsporum gypseum and 23 Nannizia cajetani. The new compounds proved to be unlikely effective in inhibiting the growth of 24 the different strains. In general the fungi parasitic on man were more sensitive than the geophilic25 species. This fact can be positive for a possible practical-therapeutic utilization of these class of 26 compounds. To verify their possible use against fungi of medical interest, the most interesting 27 substance at low doses, 6-(4-chlorophenyl)-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine, was 28 chosen to perform in vitro genotoxicity tests using: Salmonella/microsome test (SAL), Sister 29 Chromatid Excange test (SCE), Cytokinesis-Blocked Micronucleus test (CBMN) and its 30 improvement (Ara-C/CBMN). The compound showed no mutagenic activity at low doses, whereas 31 at the highest dose (100 μg/mL) it causes a generalized cytotoxic effect. The high growth inhibition32 exerted on fungi at the lowest dose and the concomitant lack of genotoxicity, at least until the dose 33 of 50 μg/mL, might suggest the compound as a safe candidate as antidermatophytic substance.
2011
34
3
324
331
Antidermatophytic activity of pyrazolo[3,4-c]isothiazoles: a preliminary approach on 4-chlorophenyl derivative for evaluation of mutagenic and clastogenic effects on bacteria and human chromosomes in vitro / D., Rossi; D., Mares; Romagnoli, Carlo; Andreotti, Elisa; S., Manfredini; C. B., Vicentini. - In: DRUG AND CHEMICAL TOXICOLOGY. - ISSN 0148-0545. - STAMPA. - 34:3(2011), pp. 324-331. [10.3109/01480545.2010.536772]
D., Rossi; D., Mares; Romagnoli, Carlo; Andreotti, Elisa; S., Manfredini; C. B., Vicentini
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/652635
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