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

J Antimicrob Chemother. 2003 Jan;51(1):167-70. doi: 10.1093/jac/dkg019.

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 > 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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Cryptococcus neoformans / drug effects*
  • Cryptococcus neoformans / isolation & purification
  • Female
  • Humans
  • Mice
  • Microbial Sensitivity Tests / statistics & numerical data
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*

Substances

  • Antifungal Agents
  • Pyrazoles
  • Thiazoles