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KMID : 0425120170550060661
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Parasites, Hosts and Diseases
2017 Volume.55 No. 6 p.661 ~ p.665
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Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin
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Park Gab-Man
Park Hyun
Oh Sang-Taek
Lee Seok-Joon
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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.
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KEYWORD
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Antimalarial activity, artemisinin, dihydroartemisinin, substituted triazolyl artemisinin, synthesis
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