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Microwave-assisted,rapid synthesis of 2-vinylquinolines and evaluation of their antimalarial activity |
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| Authors: | Guang Huang Claribel Murillo Solano Yuxin Su Nameer Ezzat Shino Matsui Liuyu Huang Debopam Chakrabarti Yu Yuan |
| Institution: | 1. Department of Chemistry, University of Central Florida, Orlando, FL, USA;2. Division of Molecular Microbiology, Burnett School of Biomedical Sciences, University of Central Florida, Orlando, FL, USA;3. Academy of Military Medical Science, Beijing, China;4. Chinese PLA Center for Disease Control and Prevention, Beijing, China |
| Abstract: | A rapid and efficient synthesis of 2-vinylquinolines via trifluoromethanesulfonamide-mediated olefination of 2-methylquinoline and aldehyde under microwave irradiation is reported. Biological evaluation of these scaffolds demonstrates that 2-vinylquinolines 3x-3z possess excellent antimalarial activities against chloroquine-resistant Dd2 strain of Plasmodium falciparum (IC50 < 100 nM). |
| Keywords: | Corresponding authors 2-Vinylquinoline 2-Methylquinoline Olefination Microwave-assisted synthesis Antimalarial |
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