Literature DB >> 9333069

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

M D Edstein1, S Bahr, B Kotecka, G D Shanks, K H Rieckmann.   

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.

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Year:  1997        PMID： 9333069      PMCID： PMC164114     

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  13 in total

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Authors:  S Thaithong; G H Beale
Journal:  Trans R Soc Trop Med Hyg       Date:  1981       Impact factor: 2.184

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Authors:  G D Shanks; M D Edstein; V Suriyamongkol; S Timsaad; H K Webster
Journal:  Am J Trop Med Hyg       Date:  1992-06       Impact factor: 2.345

3.  In vitro activities of and mechanisms of resistance to antifol antimalarial drugs.

Authors:  W K Milhous; N F Weatherly; J H Bowdre; R E Desjardins
Journal:  Antimicrob Agents Chemother       Date:  1985-04       Impact factor: 5.191

4.  The antimalarial activity of N-benzyl-oxydihydrotriazines. III. The activity of 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(2,4,5,-trichloropropyloxy)-1,3,5-triazine hydrobromide (BRL 51084) and hydrochloride (BRL 6231).

Authors:  D J Knight; P Mamalis; W Peters
Journal:  Ann Trop Med Parasitol       Date:  1982-02

5.  The antimalarial activity of N-benzyl-oxydihydrotriazines. IV. The development of resistance to BRL 6231 (4,6-diamino-1,2-dihyydro-2-,2-dimethyl-1-(2,4,5-trichloropropyloxy)-1,3,5 triazine hydrochloride) by Plasmodium berghei.

Authors:  D J Knight; P Williamson
Journal:  Ann Trop Med Parasitol       Date:  1982-02

6.  Analogues of N-benzyloxydihydrotriazines: in vitro antimalarial activity against Plasmodium falciparum.

Authors:  G E Childs; C Lambros
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7.  Malaria prophylaxis with proguanil in children living in a malaria-endemic area.

Authors:  N Limsomwong; L W Pang; P Singharaj
Journal:  Am J Trop Med Hyg       Date:  1988-03       Impact factor: 2.345

8.  Plasmodium falciparum: cloning by single-erythrocyte micromanipulation and heterogeneity in vitro.

Authors:  A M Oduola; N F Weatherly; J H Bowdre; R E Desjardins
Journal:  Exp Parasitol       Date:  1988-06       Impact factor: 2.011

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Journal:  J Parasitol       Date:  1979-06       Impact factor: 1.276

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Authors:  H K Webster; E F Boudreau; K Pavanand; K Yongvanitchit; L W Pang
Journal:  Am J Trop Med Hyg       Date:  1985-03       Impact factor: 2.345
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