Korean J Parasitol.  2005 Sep;43(3):123-126. 10.3347/kjp.2005.43.3.123.

Antimalarial activity of thiophenyl- and benzenesulfonyl-dihydroartemisinin

Affiliations
  • 1Department of Basic Science, Kwandong University College of Medicine, Gangneung 210-701, Korea. sjlee@kd.ac.kr
  • 2Department of Chemistry, Yonsei University, Wonju 220-710, Korea.
  • 3Department of Parasitology, Kwandong University College of Medicine, Gangneung 210-701, Korea.
  • 4Department of Medical Zoology, National Institute of Health, Seoul 122-201, Korea.
  • 5Department of Parasitology, Hanyang University College of Medicine, Seoul 133-791, Korea.

Abstract

Each diastereomer of 10-thiophenyl- and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10 beta-benzenesulfonyl-dihydroartemisinin showed stronger antimalarial activity than artemisinin.

Keyword

Plasmodium falciparum; antimalarial activity; artemisinin; dihydroartemisinin; synthesis; natural product

MeSH Terms

Animals
Antimalarials/chemistry/*pharmacology
Artemisinins/chemistry/*pharmacology
Chloroquine/pharmacology
Drug Resistance
Plasmodium falciparum/*drug effects
Research Support, Non-U.S. Gov't
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