Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs

  • Aoki Shin
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan Research Institute for Science and Technology (RIST), Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan Research Institute for Biomedical Sciences (RIBS), Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Tanaka Tomohiro
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Tsushima-Naka, Kita-ku, Okayama 700–8530, Japan
  • Yokoi Kenta
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Kanbe Azusa
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Morita Tomoe
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Nii Mayuka
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Satoh Hidetoshi
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Kakihana Masaki
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Otaki Shotaro
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Sekiguchi Saki
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Nakamura Koki
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Tojo Toshifumi
    Faculty of Pharmaceutical Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan Research Institute for Science and Technology (RIST), Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278–8510, Japan
  • Baba Masanori
    Division of Infection Control Research, Center for Advanced Science Research and Promotion, Kagoshima University, Kagoshima 890–8580, Japan
  • Okamoto Mika
    Division of Infection Control Research, Center for Advanced Science Research and Promotion, Kagoshima University, Kagoshima 890–8580, Japan

書誌事項

公開日
2025-04-17
資源種別
journal article
DOI
  • 10.1248/cpb.c24-00647
公開者
公益社団法人 日本薬学会

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説明

<p>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.</p>

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