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10.1016/j.bmcl.2021.128052

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2021.128052
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33887440!8055493!33887440
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suck abstract from ncbi


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pmid33887440      Bioorg+Med+Chem+Lett 2021 ; 43 (ä): 128052
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  • Development of ciclesonide analogues that block SARS-CoV-2 RNA replication #MMPMID33887440
  • Tsuji G; Yonemitsu K; Ito T; Yanase Y; Uema M; Ohoka N; Inoue T; Asakura H; Demizu Y
  • Bioorg Med Chem Lett 2021[Jul]; 43 (ä): 128052 PMID33887440show ga
  • 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.
  • |*COVID-19 Drug Treatment[MESH]
  • |COVID-19/virology[MESH]
  • |Glucocorticoids/pharmacology[MESH]
  • |Humans[MESH]
  • |Pregnenediones/*pharmacology[MESH]
  • |RNA, Viral/*antagonists & inhibitors/genetics[MESH]
  • |SARS-CoV-2/*drug effects/genetics[MESH]


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