Jung M, Li X, Bustos D A, elSohly H N, McChesney J D, Milhous W K
School of Pharmacy, University of Mississippi, University 38677.
J Med Chem. 1990 May;33(5):1516-8. doi: 10.1021/jm00167a036.
(+)-Deoxoartemisinin (2), a new and more active antimalarial agent, was successfully prepared from artemisinin in one step using NaBH4 and BF3.Et2O in THF. (-)-Deoxodeoxyartemisinin (5), a potential metabolite of deoxoartemisinin, was also prepared either from 2 or from artemisinic acid. 2 shows 8-fold increased antimalarial activity in vitro against chloroquine-resistant malaria as compared to artemisinin (1). Compound 2 possesses superior in vivo antimalarial activity to 1.
