Antimalarial Activity of C-10 Substituted Triazolyl Artemisinin.
10.3347/kjp.2017.55.6.661
- Author:
Gab Man PARK
1
;
Hyun PARK
;
Sangtae OH
;
Seokjoon LEE
Author Information
1. Department of Medical Environmental Biology, Catholic Kwandong University College of Medicine, Gangneung 25601, Korea.
- Publication Type:Brief Communication
- Keywords:
Antimalarial activity;
artemisinin;
dihydroartemisinin;
substituted triazolyl artemisinin;
synthesis
- MeSH:
Artemisinins;
Cycloaddition Reaction;
Parasites
- From:The Korean Journal of Parasitology
2017;55(6):661-665
- CountryRepublic of Korea
- Language:English
-
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.
