Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs
Shin Aoki, Tomohiro Tanaka, Kenta Yokoi, Azusa Kanbe, Tomoe Morita, Mayuka Nii, Hidetoshi Satoh, Masaki Kakihana, Shotaro Otaki, Saki Sekiguchi, Koki Nakamura, T Tojo, Masanori Baba, Mika Okamoto · Chemical and Pharmaceutical Bulletin · 2025
The pandemic of coronavirus disease 2019, caused by the new coronavirus severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), remains a serious concern worldwide. Although some effective vaccines have been developed, only a few anti-SARS-CoV-2 drugs have been approved for their clinical use. In this study, we designed and synthesized new anti-SARS-CoV-2 drugs based on the chemical structure of amodiaquine, which is known as an antimalarial drug. Consequently, we have identified amodiaquine analogs functionalized with dialkylamino-pendant aminophenol moieties that possess a high level of anti-SARS-CoV-2 activity with a low level of toxicity.