Korean J Parasitol.  2017 Dec;55(6):661-665. 10.3347/kjp.2017.55.6.661.

Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin

Affiliations
  • 1Department of Medical Environmental Biology, Catholic Kwandong University College of Medicine, Gangneung 25601, Korea.
  • 2Department of Environmental Medical Biology, Wonkwang University College of Medicine, Iksan 54538, Korea.
  • 3Department of Basic Science, Catholic Kwandong University College of Medicine, Gangneung 25601, Korea.
  • 4Department of Pharmacology, Catholic Kwandong University College of Medicine, Gangneung 25601, Korea. sjlee@cku.ac.kr

Abstract

We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial activities than those shown by the derivatives having electron-donating groups. In particularly, m-chlorotriazolyl artemisinin (9d-12d) showed antimalarial activity equivalent to that of artemisinin and could be a strong drug candidate.

Keyword

Antimalarial activity; artemisinin; dihydroartemisinin; substituted triazolyl artemisinin; synthesis

MeSH Terms

Artemisinins
Cycloaddition Reaction
Parasites
Artemisinins
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