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

Author:

Edstein M D1,Bahr S1,Kotecka B1,Shanks G D1,Rieckmann K H1

Affiliation:

1. Australian Army Malaria Institute, Brisbane.

Abstract

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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference17 articles.

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5. Anti-Pneumocystis carinii activity of PS-15, a new biguanide folate antagonist;Hughes W. T.;Antimicrob. Agents Chemother.,1993

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