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Challenges Based on Antiplasmodial and Antiviral Activities of 7-Chloro-4-aminoquinoline Derivatives. 2023
Satoshi Mizuta, and
Farhana Mosaddeque, and
Mya Myat Ngwe Tun, and
Awet Alem Teklemichael, and
Mayumi Taniguchi, and
Masashi Hosokawa, and
Tomoko Yamaguchi, and
Juliann Makau, and
Nguyen Tien Huy, and
Shusaku Mizukami, and
Noriyuki Nishida, and
Kouichi Morita, and
Kenji Hirayama
Center for Bioinformatics and Molecular Medicine, Nagasaki University, 1-14 Bunkyo, 852-8521, Nagasaki, Japan.
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.
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