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Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Bioorg+Med+Chem+Lett 2021 ; 43 (ä): 128052 Nephropedia Template TP
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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.