Development of ciclesonide analogues that block SARS-CoV-2 RNA replication

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) gen...

Descripción completa

Detalles Bibliográficos
Autores principales: Tsuji, Genichiro, Yonemitsu, Kenzo, Ito, Takahito, Yanase, Yuta, Uema, Masashi, Ohoka, Nobumichi, Inoue, Takao, Asakura, Hiroshi, Demizu, Yosuke
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8055493/
https://www.ncbi.nlm.nih.gov/pubmed/33887440
http://dx.doi.org/10.1016/j.bmcl.2021.128052
Descripción
Sumario: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.

Ejemplares similares