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Development of ciclesonide analogues that block SARS-CoV-2 RNA replication.
Tsuji, Genichiro; Yonemitsu, Kenzo; Ito, Takahito; Yanase, Yuta; Uema, Masashi; Ohoka, Nobumichi; Inoue, Takao; Asakura, Hiroshi; Demizu, Yosuke.
  • Tsuji G; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
  • Yonemitsu K; Division of Biomedical Food Research, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
  • Ito T; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
  • Yanase Y; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan; Graduate School of Medical Life Science, Yokohama City University, 1-7-29, Yokohama, Kanagawa 230-0045, Japan.
  • Uema M; Division of Biomedical Food Research, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
  • Ohoka N; Division of Molecular Target and Gene Therapy Products, National Institute of Health Sciences, 3-25-26, Tonomachi, 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, Kanagawa 210-9501, Japan.
  • Asakura H; Division of Biomedical Food Research, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
  • Demizu Y; Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, 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.
Bioorg Med Chem Lett ; 43: 128052, 2021 07 01.
Article in English | MEDLINE | ID: covidwho-1196690
ABSTRACT
Ciclesonide is an inhaled corticosteroid used to treat asthma and is currently undergoing clinical trials for treatment of coronavirus disease 2019 (COVID-19). An active metabolite of ciclesonide, Cic2, was recently reported to repress severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) genomic RNA replication. Herein, we designed and synthesized a few types of ciclesonide analogues. Cic4 (bearing an azide group) and Cic6 (bearing a chloro group) potently decreased SARS-CoV-2 viral replication and had low cytotoxicity compared with Cic2 (bearing a hydroxy group). These compounds are promising as novel therapeutic agents for COVID-19 that show significant antiviral activity.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Pregnenediones / RNA, Viral / SARS-CoV-2 / COVID-19 Drug Treatment Type of study: Prognostic study Limits: Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2021 Document Type: Article Affiliation country: J.bmcl.2021.128052

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Pregnenediones / RNA, Viral / SARS-CoV-2 / COVID-19 Drug Treatment Type of study: Prognostic study Limits: Humans Language: English Journal: Bioorg Med Chem Lett Journal subject: Biochemistry / Chemistry Year: 2021 Document Type: Article Affiliation country: J.bmcl.2021.128052