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1.
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.


Subject(s)
Antiviral Agents , COVID-19 , Acetals/pharmacology , Antiviral Agents/pharmacology , COVID-19/drug therapy , Humans , Pregnenediones , RNA, Viral/genetics , RNA, Viral/pharmacology , SARS-CoV-2 , Virus Replication/genetics
2.
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.


Subject(s)
COVID-19/drug therapy , Pregnenediones/pharmacology , RNA, Viral/antagonists & inhibitors , SARS-CoV-2/drug effects , COVID-19/virology , Glucocorticoids/pharmacology , Humans , RNA, Viral/genetics , SARS-CoV-2/genetics , Virus Replication/genetics
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