Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs
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.
Authors
- Azusa Kanbe
- Shin Aoki (ORCID: https://orcid.org/0000-0002-4287-6487)
- Masaki Kakihana
- Tomoya Morita (ORCID: https://orcid.org/0000-0003-2798-5113)
- T Tojo (ORCID: https://orcid.org/0000-0003-3803-8824)
- Kenta Yokoi (ORCID: https://orcid.org/0000-0002-3437-4567)
- Koki Nakamura (ORCID: https://orcid.org/0000-0002-3036-234X)
- Masanori Baba (ORCID: https://orcid.org/0000-0002-6109-5248)
- Mika Okamoto (ORCID: https://orcid.org/0009-0001-4247-6635)
- Tomohiro Tanaka
- Hidetoshi Satoh
- Mayuka Nii
- S Sekiguchi
- Shotaro Otaki
Institutions
- Kagoshima University (JP)
- Tokyo University of Science (JP)
- Okayama University (JP)
Publication Details
- Journal
- Chemical and Pharmaceutical Bulletin
- Published
- 2025-04-16
- DOI
- https://doi.org/10.1248/cpb.c24-00647
- Primary Topic
- Computational Drug Discovery Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Japan Agency for Medical Research and Development
- Ministry of Education, Culture, Sports, Science and Technology
- Research Promotion Foundation
- Shionogi