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RESEARCH PRODUCT

In vitro and in vivo anticryptococcal activities of a new pyrazolo-isothiazole derivative

Giovanni M. GiammancoAnna Maria SchimizziGiuseppe PizzoD. ArzeniFrancesco BarchiesiMaria Eleonora MiliciMaurizio ManfriniGiorgio ScaliseChiara Beatrice VicentiniDaniele Giannini

subject

Microbiology (medical)Settore MED/07 - Microbiologia E Microbiologia ClinicaAntifungal AgentsRatónMicrobial Sensitivity TestsPharmacologyMicechemistry.chemical_compoundOral administrationIn vivomedicineAnimalsHumansPharmacology (medical)Cryptococcus neoformansPharmacologyIsothiazolebiologyFungi imperfectibiology.organism_classificationmedicine.diseaseIn vitroThiazolesInfectious DiseaseschemistryCryptococcosisImmunologyCryptococcus neoformansPyrazolesFemale

description

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 > or =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.

10.1093/jac/dkg019http://hdl.handle.net/11392/1210482