Abstract
The in vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline was compared against chloroquine-resistant and -susceptible strains of Plasmodium falciparum using a semi-micro drug susceptibility test. For each strain, the corresponding enantiomers exhibited similar activities. The enantiomers of halofantrine were the most active against both susceptible and resistant strains, followed by the enantiomers of mefloquine and enpiroline.
Full text
PDF



Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Carroll F. I., Berrang B., Linn C. P. Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid. J Med Chem. 1978 Apr;21(4):326–330. doi: 10.1021/jm00202a002. [DOI] [PubMed] [Google Scholar]
- Carroll F. I., Blackwell J. T. Optical isomers of aryl-2-piperidylmethanol antimalarial agents. Preparation, optical purity, and absolute stereochemistry. J Med Chem. 1974 Feb;17(2):210–219. doi: 10.1021/jm00248a015. [DOI] [PubMed] [Google Scholar]
- Cosgriff T. M., Boudreau E. F., Pamplin C. L., 3rd, Berman J. D., Shmuklarsky M. J., Canfield C. J. Evaluation of the 4-pyridinemethanol WR 180,409 (enpiroline) in the treatment of induced Plasmodium falciparum infections in healthy, non-immune subjects. Am J Trop Med Hyg. 1984 Sep;33(5):767–771. doi: 10.4269/ajtmh.1984.33.767. [DOI] [PubMed] [Google Scholar]
- Desjardins R. E., Canfield C. J., Haynes J. D., Chulay J. D. Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique. Antimicrob Agents Chemother. 1979 Dec;16(6):710–718. doi: 10.1128/aac.16.6.710. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Fu S., Björkman A., Wåhlin B., Ofori-Adjei D., Ericsson O., Sjöqvist F. In vitro activity of chloroquine, the two enantiomers of chloroquine, desethylchloroquine and pyronaridine against Plasmodium falciparum. Br J Clin Pharmacol. 1986 Jul;22(1):93–96. [PMC free article] [PubMed] [Google Scholar]
- Gimenez F., Farinotti R., Thuillier A., Hazebroucq G., Wainer I. W. Determination of the enantiomers of mefloquine in plasma and whole blood using a coupled achiral-chiral high-performance liquid chromatographic system. J Chromatogr. 1990 Aug 3;529(2):339–346. doi: 10.1016/s0378-4347(00)83840-2. [DOI] [PubMed] [Google Scholar]
- Karle J. M., Karle I. L. Crystal and molecular structure of the antimalarial agent enpiroline. Antimicrob Agents Chemother. 1989 Jul;33(7):1081–1089. doi: 10.1128/aac.33.7.1081. [DOI] [PMC free article] [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]
- Schmidt L. H., Crosby R., Rasco J., Vaughan D. Antimalarial activities of various 4-quinolonemethanols with special attention to WR-142,490 (mefloquine). Antimicrob Agents Chemother. 1978 Jun;13(6):1011–1030. doi: 10.1128/aac.13.6.1011. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Trager W., Jensen J. B. Human malaria parasites in continuous culture. Science. 1976 Aug 20;193(4254):673–675. doi: 10.1126/science.781840. [DOI] [PubMed] [Google Scholar]
- Wesche D. L., Black J. A comparison of the antimalarial activity of the cinchona alkaloids against Plasmodium falciparum in vitro. J Trop Med Hyg. 1990 Jun;93(3):153–159. [PubMed] [Google Scholar]