Parasites, Hosts and Diseases

  • 제55권6호
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  • Pages.661-665
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  • 2017
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  • 2982-5164(pISSN)
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  • 1738-0006(eISSN)
대한기생충학·열대의학회 (The Korea Society for Parasitology and Tropical Medicine)
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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)
  • 투고 : 2017.08.08
  • 심사 : 2017.12.05
  • 발행 : 2017.12.31
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초록

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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참고문헌

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