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Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: Design,synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition |
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| Authors: | Rita Capela Rudi Oliveira Lídia M. Gonçalves Ana Domingos Jiri Gut Philip J. Rosenthal Francisca Lopes Rui Moreira |
| Affiliation: | 1. iMed.UL, Faculty of Pharmacy, University of Lisbon, Av Prof. Gama Pinto, 1649-003, Portugal;2. CMDT, IHMT, Universidade Nova de Lisboa, R. Junqueira 96, 1349-008 Lisboa, Portugal;3. Department of Medicine, San Francisco General Hospital, University of California, San Francisco, Box 0811, San Francisco, CA 94143, USA |
| Abstract: | A series of artemisinin–vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range. |
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