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Synthesis of 11-aza-artemisinin derivatives using the Ugi reaction and an evaluation of their antimalarial activity |
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| Authors: | Thanh Nguyen Le Wim M De Borggraeve Philippe Grellier Van Cuong Pham Wim Dehaen Van Hung Nguyen |
| Institution: | 1. Institute of Marine Biochemistry—Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet Road, Cau Giay, Hanoi, Viet Nam;2. Department of Chemistry, KU Leuven, Celestijnenlaan 200F—bus 2404, B-3001 Leuven, Belgium;3. Muséum National d’Histoire Naturelle, 63 rue Buffon, 75005 Paris, France |
| Abstract: | A series of new 11-aza-artemisinin derivatives were prepared from 11-aza-artemisinin using the Ugi reaction. An antimalarial activity evaluation against the FcB1 strain indicated that compounds 7, 10, and 16 had very strong inhibitory activity. Comparison of the activity among the synthetic derivatives of this series revealed that the length of the side chain R group on the amide nitrogen could be critical for their antimalarial properties. |
| Keywords: | Artemisinin Aza-artemisinin Ugi reaction Antimalarial Synthesis |
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