This Article
Right arrow Full Text (PDF)
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrowReprints and Permissions
Right arrow Copyright Information
Right arrow Books from ASM Press
Right arrow MicrobeWorld
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Edstein, M. D.
Right arrow Articles by Rieckmann, K. H.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Edstein, M. D.
Right arrow Articles by Rieckmann, K. H.

 Previous Article  |  Next Article 

Antimicrob. Agents Chemother., Oct 1997, 2300-2301, Vol 41, No. 10
Copyright © 1997 by the American Society for Microbiology. All rights reserved.

In vitro activities of the biguanide PS-15 and its metabolite, WR99210, against cycloguanil-resistant Plasmodium falciparum isolates from Thailand

MD Edstein, S Bahr, B Kotecka, GD Shanks and KH Rieckmann
Australian Army Malaria Institute, Brisbane.

The in vitro activities of the new biguanide PS-15 and its putative active metabolite, WR99210, were determined against seven different isolates or clones of Plasmodium falciparum. The mean 50% inhibitory concentrations of PS-15 and WR99210 were 1,015 and 0.06 ng/ml, respectively. WR99210 was up to 363 times more potent than cycloguanil, the active metabolite of proguanil, against cycloguanil-resistant parasites. The pronounced activity of WR99210 against multidrug- resistant P. falciparum indicates that further studies are required to determine the value of the prodrug, PS-15, as an antimalarial agent.


This article has been cited by other articles:

  • Edstein, M. D., Kotecka, B. M., Ager, A. L., Smith, K. S., DiTusa, C. A., Diaz, D. S., Kyle, D. E., Schiehser, G. A., Jacobus, D. P., Rieckmann, K. H., O'Neil, M. T. (2007). Antimalarial pharmacodynamics and pharmacokinetics of a third-generation antifolate JPC2056 in cynomolgus monkeys using an in vivo in vitro model. J Antimicrob Chemother 60: 811-818 [Abstract] [Full Text]  
  • Nzila, A. (2006). The past, present and future of antifolates in the treatment of Plasmodium falciparum infection. J Antimicrob Chemother 57: 1043-1054 [Abstract] [Full Text]