Abstract
The in vitro activity of cycloguanil was assessed against 86 African isolates of Plasmodium falciparum by a semi-micro assay system. A bimodal distribution of susceptibility patterns was observed, with 44% of the isolates being cycloguanil susceptible. Cycloguanil alone retains a high activity against the intraerythrocytic forms of some isolates and, together with its activity against the hepatic stages, may be useful for chemoprophylaxis when combined with chloroquine.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Eriksson B., Courtier B., Bjorkman A., Miltgen F., Mazier D. Activity of dihydrofolate reductase inhibitors on the hepatic stages of Plasmodium yoelii yoelii in vitro. Trans R Soc Trop Med Hyg. 1991 Nov-Dec;85(6):725–726. doi: 10.1016/0035-9203(91)90429-3. [DOI] [PubMed] [Google Scholar]
- Fisk T. L., Millet P., Collins W. E., Nguyen-Dinh P. In vitro activity of antimalarial compounds on the exoerythrocytic stages of Plasmodium cynomolgi and P. knowlesi. Am J Trop Med Hyg. 1989 Mar;40(3):235–239. doi: 10.4269/ajtmh.1989.40.235. [DOI] [PubMed] [Google Scholar]
- Foote S. J., Galatis D., Cowman A. F. Amino acids in the dihydrofolate reductase-thymidylate synthase gene of Plasmodium falciparum involved in cycloguanil resistance differ from those involved in pyrimethamine resistance. Proc Natl Acad Sci U S A. 1990 Apr;87(8):3014–3017. doi: 10.1073/pnas.87.8.3014. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Gozal D., Hengy C., Fadat G. Prolonged malaria prophylaxis with chloroquine and proguanil (chloroguanide) in a nonimmune resident population of an endemic area with a high prevalence of chloroquine resistance. Antimicrob Agents Chemother. 1991 Feb;35(2):373–376. doi: 10.1128/aac.35.2.373. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Howells R. E., Gilles H. M., Bent N. S. A comparison of the pyrimethamine and cycloguanil sensitivities of the pre-erythrocytic and erythrocytic stages of drug-sensitive and -resistant strains of Plasmodium yoelii. Ann Trop Med Parasitol. 1985 Jun;79(3):247–251. doi: 10.1080/00034983.1985.11811915. [DOI] [PubMed] [Google Scholar]
- Le Bras J., Deloron P. In vitro study of drug sensitivity of Plasmodium falciparum: evaluation of a new semi-micro test. Am J Trop Med Hyg. 1983 May;32(3):447–451. doi: 10.4269/ajtmh.1983.32.447. [DOI] [PubMed] [Google Scholar]
- Petersen E., Hogh B., Hanson A. P., Bjorkman A., Flacks H. In vitro and in vivo susceptibility of Plasmodium falciparum isolates from Liberia to pyrimethamine, cycloguanil and chlorcycloguanil. Ann Trop Med Parasitol. 1990 Dec;84(6):563–571. doi: 10.1080/00034983.1990.11812511. [DOI] [PubMed] [Google Scholar]
- Peterson D. S., Milhous W. K., Wellems T. E. Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria. Proc Natl Acad Sci U S A. 1990 Apr;87(8):3018–3022. doi: 10.1073/pnas.87.8.3018. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Watkins W. M., Howells R. E., Brandling-Bennett A. D., Koech D. K. In vitro susceptibility of Plasmodium falciparum isolates from Jilore, Kenya, to antimalarial drugs. Am J Trop Med Hyg. 1987 Nov;37(3):445–451. doi: 10.4269/ajtmh.1987.37.445. [DOI] [PubMed] [Google Scholar]
- Watkins W. M., Sixsmith D. G., Chulay J. D. The activity of proguanil and its metabolites, cycloguanil and p-chlorophenylbiguanide, against Plasmodium falciparum in vitro. Ann Trop Med Parasitol. 1984 Jun;78(3):273–278. doi: 10.1080/00034983.1984.11811816. [DOI] [PubMed] [Google Scholar]