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1,2,4-Trioxanes as potential antimalarial agents.

Publication ,  Journal Article
Kepler, JA; Philip, A; Lee, YW; Morey, MC; Carroll, FI
Published in: J Med Chem
April 1988

A number of 1,2,4-trioxanes were prepared and tested for antimalarial activity in search of a simplified analogue of the naturally occurring antimalarial qinghaosu. The compounds were assayed in an in vitro system for antimalarial activity against chloroquine-susceptible and chloroquine-resistant strains of Plasmodium falciparum. The most active compounds were methyl 2-(2,4a-epidioxy-4a,5,6,7,8,8a-hexahydro-5,5,8a-trimethyl-2H-1-benzop yra n-2-yl) acetate (3b), which showed IC20's of 96 and 39 ng/mL, respectively, and 2,4a-epidioxy-3,4,4a,5,6,7,8,8a-octahydro-2-[2-(benzoyloxy)propyl]-5,5,8 a- trimethyl-2H-1-benzopyran (12), which showed IC50's of 24 and 99 ng/mL, respectively. For comparison, qinghaosu exhibits an IC50 of 1 ng/mL for both strains.

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Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

April 1988

Volume

31

Issue

4

Start / End Page

713 / 716

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Sesquiterpenes
  • Plasmodium falciparum
  • Plasmodium berghei
  • Mice
  • Medicinal & Biomolecular Chemistry
  • Malaria
  • Drug Resistance
  • Chloroquine
  • Artemisinins
 

Citation

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Kepler, J. A., Philip, A., Lee, Y. W., Morey, M. C., & Carroll, F. I. (1988). 1,2,4-Trioxanes as potential antimalarial agents. J Med Chem, 31(4), 713–716. https://doi.org/10.1021/jm00399a004
Kepler, J. A., A. Philip, Y. W. Lee, M. C. Morey, and F. I. Carroll. “1,2,4-Trioxanes as potential antimalarial agents.J Med Chem 31, no. 4 (April 1988): 713–16. https://doi.org/10.1021/jm00399a004.
Kepler JA, Philip A, Lee YW, Morey MC, Carroll FI. 1,2,4-Trioxanes as potential antimalarial agents. J Med Chem. 1988 Apr;31(4):713–6.
Kepler, J. A., et al. “1,2,4-Trioxanes as potential antimalarial agents.J Med Chem, vol. 31, no. 4, Apr. 1988, pp. 713–16. Pubmed, doi:10.1021/jm00399a004.
Kepler JA, Philip A, Lee YW, Morey MC, Carroll FI. 1,2,4-Trioxanes as potential antimalarial agents. J Med Chem. 1988 Apr;31(4):713–716.
Journal cover image

Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

April 1988

Volume

31

Issue

4

Start / End Page

713 / 716

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Sesquiterpenes
  • Plasmodium falciparum
  • Plasmodium berghei
  • Mice
  • Medicinal & Biomolecular Chemistry
  • Malaria
  • Drug Resistance
  • Chloroquine
  • Artemisinins