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http://dx.doi.org/10.3347/kjp.2017.55.6.661

Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin  

Park, Gab-Man (Department of Medical Environmental Biology, Catholic Kwandong University College of Medicine)
Park, Hyun (Department of Environmental Medical Biology, Wonkwang University College of Medicine)
Oh, Sangtae (Department of Basic Science, Catholic Kwandong University College of Medicine)
Lee, Seokjoon (Department of Pharmacology, Catholic Kwandong University College of Medicine)
Publication Information
Parasites, Hosts and Diseases / v.55, no.6, 2017 , pp. 661-665 More about this Journal
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.
Keywords
Antimalarial activity; artemisinin; dihydroartemisinin; substituted triazolyl artemisinin; synthesis;
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