Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Tsuji, Genichiro, Nakajima, Shogo, Watashi, Koichi, Torii, Shiho, Suzuki, Rigel, Fukuhara, Takasuke, Ohoka, Nobumichi, Inoue, Takao, Demizu, Yosuke
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society. 2022
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9014634/
https://www.ncbi.nlm.nih.gov/pubmed/35641031
http://dx.doi.org/10.1016/j.jphs.2022.04.001
_version_ 1784688224378028032
author Tsuji, Genichiro
Nakajima, Shogo
Watashi, Koichi
Torii, Shiho
Suzuki, Rigel
Fukuhara, Takasuke
Ohoka, Nobumichi
Inoue, Takao
Demizu, Yosuke
author_facet Tsuji, Genichiro
Nakajima, Shogo
Watashi, Koichi
Torii, Shiho
Suzuki, Rigel
Fukuhara, Takasuke
Ohoka, Nobumichi
Inoue, Takao
Demizu, Yosuke
author_sort Tsuji, Genichiro
collection PubMed
description 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.
format Online
Article
Text
id pubmed-9014634
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society.
record_format MEDLINE/PubMed
spelling pubmed-90146342022-04-18 Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication Tsuji, Genichiro Nakajima, Shogo Watashi, Koichi Torii, Shiho Suzuki, Rigel Fukuhara, Takasuke Ohoka, Nobumichi Inoue, Takao Demizu, Yosuke J Pharmacol Sci Short Communication 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. The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society. 2022-07 2022-04-18 /pmc/articles/PMC9014634/ /pubmed/35641031 http://dx.doi.org/10.1016/j.jphs.2022.04.001 Text en © 2022 The Authors Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Short Communication
Tsuji, Genichiro
Nakajima, Shogo
Watashi, Koichi
Torii, Shiho
Suzuki, Rigel
Fukuhara, Takasuke
Ohoka, Nobumichi
Inoue, Takao
Demizu, Yosuke
Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title_full Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title_fullStr Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title_full_unstemmed Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title_short Antiviral activity of ciclesonide acetal derivatives blocking SARS-CoV-2 RNA replication
title_sort antiviral activity of ciclesonide acetal derivatives blocking sars-cov-2 rna replication
topic Short Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9014634/
https://www.ncbi.nlm.nih.gov/pubmed/35641031
http://dx.doi.org/10.1016/j.jphs.2022.04.001
work_keys_str_mv AT tsujigenichiro antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT nakajimashogo antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT watashikoichi antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT toriishiho antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT suzukirigel antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT fukuharatakasuke antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT ohokanobumichi antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT inouetakao antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication
AT demizuyosuke antiviralactivityofciclesonideacetalderivativesblockingsarscov2rnareplication

Ejemplares similares