IN-VITRO ACTIVITIES OF THE BIGUANIDE PS-15 AND ITS METABOLITE, WR99210, AGAINST CYCLOGUANIL-RESISTANT PLASMODIUM-FALCIPARUM ISOLATES FROM THAILAND

Authors
EDSTEIN MD BAHR S KOTECKA B SHANKS GD RIECKMANN KH
Citation
Md. Edstein et al., IN-VITRO ACTIVITIES OF THE BIGUANIDE PS-15 AND ITS METABOLITE, WR99210, AGAINST CYCLOGUANIL-RESISTANT PLASMODIUM-FALCIPARUM ISOLATES FROM THAILAND, Antimicrobial agents and chemotherapy, 41(10), 1997, pp. 2300-2301
Citations number
17
Categorie Soggetti
Pharmacology & Pharmacy",Microbiology
Journal title
Antimicrobial agents and chemotherapy → ACNP
ISSN journal
00664804
Volume
41
Issue
10
Year of publication
1997
Pages
2300 - 2301
Database
ISI
SICI code
0066-4804(1997)41:10<2300:IAOTBP>2.0.ZU;2-M
Abstract
The in vitro activities of the new biguanide PS-15 and its putative ac tive metabolite, WR99210, were determined against seven different isol ates or clones of Plasmodium falciparum. The mean 50% inhibitory conce ntrations 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. falcipa rum indicates that further studies are required to determine the value of the prodrug, PS-15, as an antimalarial agent.