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JAC Advance Access originally published online on November 28, 2002
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Journal of Antimicrobial Chemotherapy (2003) 51, 167-170
© 2003 The British Society for Antimicrobial Chemotherapy

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

Francesco Barchiesi1,*, Maria E. Milici2, Daniela Arzeni1, Anna M. Schimizzi1, Giuseppe Pizzo3, Giovanni M. Giammanco2, Daniele Giannini4, Maurizio Manfrini5, Giorgio Scalise1 and Chiara B. Vicentini5

1 Istituto di Malattie Infettive e Medicina Pubblica, Università degli Studi di Ancona, Azienda Ospedaliera Umberto I°, Via Conca 60020, Torrette di Ancona, Ancona; 2 Dipartimento di Igiene e Microbiologia, Università di Palermo, Palermo; 3 Dipartimento di Discipline Odontostomatologiche, Università di Palermo, Palermo; 4 Centro di Gestione Presidenza Medicina e Chirurgia, Università di Ancona, Ancona; 5 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Ferrara, Italy

Received 2 January 2002; returned 4 June 2002; revised 18 June 2002; accepted 27 September 2002

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.

* Corresponding author. Tel: +39-071-596-3467; Fax: +39-071-596-3468; E-mail: cmalinf{at}popcsi.unian.it


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