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Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication.
Tsuji, Genichiro; Nakajima, Shogo; Watashi, Koichi; Torii, Shiho; Suzuki, Rigel; Fukuhara, Takasuke; Ohoka, Nobumichi; Inoue, Takao; Demizu, Yosuke.
  • Tsuji G; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki, Kanagawa, 210-9501, Japan. Electronic address: gtsuji@nihs.go.jp.
  • Nakajima S; National Institute of Infectious Diseases, Research Center for Drug and Vaccine Development, 1-23-1 Toyama, Shinjuku-ku, Tokyo, 162-8640, Japan; National Institute of Infectious Diseases, Department of Virology II, 1-23-1 Toyama, Shinjuku-ku, Tokyo, 162-8640, Japan; Choju Medical Institute, 19-14 Ya
  • Watashi K; National Institute of Infectious Diseases, Research Center for Drug and Vaccine Development, 1-23-1 Toyama, Shinjuku-ku, Tokyo, 162-8640, Japan; National Institute of Infectious Diseases, Department of Virology II, 1-23-1 Toyama, Shinjuku-ku, Tokyo, 162-8640, Japan; Department of Applied Biological
  • Torii S; Laboratory of Virus Control, Research Institute for Microbial Diseases, Osaka University, Suita, 565-0871, Japan; Insect-Virus Interactions Unit, Department of Virology, Institute Pasteur, Paris, 75015, France.
  • Suzuki R; Department of Microbiology and Immunology, Graduate School of Medicine, Hokkaido University, N-15, W-7, Kita-ku, Sapporo, Hokkaido, 060-8638, Japan.
  • Fukuhara T; Department of Microbiology and Immunology, Graduate School of Medicine, Hokkaido University, N-15, W-7, Kita-ku, Sapporo, Hokkaido, 060-8638, Japan.
  • Ohoka N; Division of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki, Kanagawa, 210-9501, Japan.
  • Inoue T; Division of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki, Kanagawa, 210-9501, Japan.
  • Demizu Y; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26 Tonomachi, Kawasaki-ku, Kawasaki, Kanagawa, 210-9501, Japan; Graduate School of Medical Life Science, Yokohama City University, 1-7-29, Yokohama, Kanagawa, 230-0045, Japan. Electronic address: demizu@nihs.go.jp.
J Pharmacol Sci ; 149(3): 81-84, 2022 Jul.
Article in English | MEDLINE | ID: covidwho-1796436
ABSTRACT
Ciclesonide (Cic) is approved as an inhalant for asthma and was clinically tested as a candidate therapy for coronavirus disease 2019 (COVID-19). Its active metabolite Cic2 was recently reported to suppress genomic RNA replication of severe acute respiratory syndrome coronavirus 2. In this study, we designed and synthesized a set of ciclesonide-acetal (Cic-acetal) derivatives. Among designated compounds, some Cic-acetal derivatives with a linear alkyl chain exhibited strong viral copy-number reduction activities compared with Cic2. These compounds might serve as lead compounds for developing novel anti-COVID-19 agents.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / COVID-19 Drug Treatment Type of study: Prognostic study Limits: Humans Language: English Journal: J Pharmacol Sci Journal subject: Pharmacology Year: 2022 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / COVID-19 Drug Treatment Type of study: Prognostic study Limits: Humans Language: English Journal: J Pharmacol Sci Journal subject: Pharmacology Year: 2022 Document Type: Article