SYNTHESIS AND IN-VIVO ANTIMALARIAL ACTIVITY OF 12-ALPHA-TRIFLUOROMETHYL-HYDROARTEMISININ

Authors
ABOUABDELLAH A BEGUE JP BONNETDELPON D GANTIER JC NGA TTT THAC TD
Citation
A. Abouabdellah et al., SYNTHESIS AND IN-VIVO ANTIMALARIAL ACTIVITY OF 12-ALPHA-TRIFLUOROMETHYL-HYDROARTEMISININ, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2717-2720
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2717 - 2720
Database
ISI
SICI code
0960-894X(1996)6:22<2717:SAIAAO>2.0.ZU;2-0
Abstract
12 alpha-Trifluoromethyl-hydroartemisinin 4 was selectively prepared f rom the reaction of artemisinin 1 with TMSCF(3) in good yields. The al pha configuration of the CF3 substituent was established by NMR experi ments. Compound 4 exhibits a better antimalarial activity against Plas modium vinckei in mice, than artemisinin. Copyright (C) 1996 Elsevier Science Ltd