We investigated the activity of a pyrazolo-isothiazole derivative (G8) against Cryptococcus neoformans. A first screening test showed that G8 at 10 mg/L inhibited the growth of 14 of 15 clinical isolates tested. Killing experiments showed that fungicidal activity was achieved after 8 h of treatment with G8 at concentrations ≥10 mg/L. In a murine model of systemic cryptococcosis, G8 was effective at prolonging survival compared with the controls. Our data indicate that this new derivative has a potential therapeutic role in infections caused by C. neoformans.
Barchiesi, F., Milici, M.E., Arzeni, D., Schimizzi, A.M., Pizzo, G., Giammanco, G., et al. (2003). In vitro and in vivo anticryptococcal activities of a new pyrazolo-isothiazole derivative. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 51(1), 167-170 [10.1093/jac/dkg019].
In vitro and in vivo anticryptococcal activities of a new pyrazolo-isothiazole derivative
Milici, Maria E.;Pizzo, Giuseppe;Giammanco, Giovanni;
2003-01-01
Abstract
We investigated the activity of a pyrazolo-isothiazole derivative (G8) against Cryptococcus neoformans. A first screening test showed that G8 at 10 mg/L inhibited the growth of 14 of 15 clinical isolates tested. Killing experiments showed that fungicidal activity was achieved after 8 h of treatment with G8 at concentrations ≥10 mg/L. In a murine model of systemic cryptococcosis, G8 was effective at prolonging survival compared with the controls. Our data indicate that this new derivative has a potential therapeutic role in infections caused by C. neoformans.
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