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Challenges Based on Antiplasmodial and Antiviral Activities of 7-Chloro-4-aminoquinoline Derivatives |
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| Authors: | Dr Satoshi Mizuta Dr Farhana Mosaddeque Dr Mya Myat Ngwe Tun Dr Awet Alem Teklemichael Mayumi Taniguchi Masashi Hosokawa Tomoko Yamaguchi Dr Juliann Makau Dr Nguyen Tien Huy Dr Shusaku Mizukami Prof Noriyuki Nishida Prof Kouichi Morita Prof Kenji Hirayama |
| Affiliation: | 1. Center for Bioinformatics and Molecular Medicine, Nagasaki University, 1-14 Bunkyo, 852-8521 Nagasaki, Japan;2. Department of Immunogenetics Institute of Tropical Medicine (NEKKEN), Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan;3. Department of Virology Institute of Tropical Medicine (NEKKEN), Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan;4. Department of Immune Regulation Shionogi Global Infectious Diseases Division, Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan;5. School of Medicine, Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan;6. Center for Virus Research, Kenya Medical Research Institute, 54840-00200 Nairobi, Kenya;7. Department of Immunogenetics Institute of Tropical Medicine (NEKKEN), Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan
School of Tropical Medicine and Global Health, Nagasaki University, 1-12-4 Sakamoto, 852-8102>8. Nagasaki, Japan;9. Department of Molecular Microbiology and Immunology, Nagasaki University, 1-12-4 Sakamoto, 852-8102 Nagasaki, Japan;10. Department of Virology Institute of Tropical Medicine (NEKKEN), Nagasaki University, 1-12-4 Sakamoto, 852-8523 Nagasaki, Japan Dejima Infectious Disease Research Alliance, Nagasaki University, Nagasaki, 852-8523 Japan |
| Abstract: | We report the structural functionalization of the terminal amino group of N1-(7-chloroquinolin-4-yl) butane-1,4-diamine, leading to a series of 7-chloro-4-aminoquinoline derivatives, and their evaluation as potent anti-malarial and anti-viral agents. Some compounds exhibited promising anti-malarial effects against the Plasmodium falciparum 3D7 (chloroquine-sensitive) and Dd2 (chloroquine-resistant) strains. In addition, these compounds were assayed in vitro against influenza A virus (IAV) and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Compound 5 h , bearing an N-mesityl thiourea group, displayed pronounced anti-infectious effects against malaria, IAV, and SARS-CoV-2. These results provide new insights into drug discovery for the prevention or treatment of malaria and virus co-infection. |
| Keywords: | Chloroquine Anti-malaria Anti-influenza virus Anti-SARS-CoV-2 Co-infection |