Parasites, Hosts and Diseases

"substituted triazolyl artemisinin"

Brief Communication

Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin: Gab-Man Park, Hyun Park, Sangtae Oh, Seokjoon Lee; Korean J Parasitol 2017;55(6):661-665.
Published online December 31, 2017; DOI: https://doi.org/10.3347/kjp.2017.55.6.661

Abstract
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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.

Citations

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