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

被引：5

作者：

Tsuji, Genichiro ^{[1
]}

Nakajima, Shogo ^{[2
,3
,4
]}

Watashi, Koichi ^{[2
,3
,5
]}

Torii, Shiho ^{[6
,7
]}

Suzuki, Rigel ^{[8
]}

Fukuhara, Takasuke ^{[8
]}

Ohoka, Nobumichi ^{[9
]}

Inoue, Takao ^{[9
]}

Demizu, Yosuke ^{[1
,10
]}

机构：

[1] Natl Inst Hlth Sci, Div Organ Chem, Kawasaki Ku, 3-25-26 Tonomachi, Kawasaki, Kanagawa 2109501, Japan

[2] Natl Inst Infect Dis, Res Ctr Drug & Vaccine Dev, Shinjuku Ku, 1-23-1 Toyama, Tokyo 1628640, Japan

[3] Natl Inst Infect Dis, Dept Virol 2, Shinjuku Ku, 1-23-1 Toyama, Tokyo 1628640, Japan

[4] Choju Med Inst, 19-14 Yamanaka, Toyohashi, Aichi 4418124, Japan

[5] Tokyo Univ Sci, Dept Appl Biol Sci, 2641 Yamazaki, Noda, Chiba 2788510, Japan

[6] Osaka Univ, Microbial Dis Res Inst, Lab Virus Control, Suita, Osaka 5650871, Japan

[7] Inst Pasteur, Dept Virol, Insect Virus Interact Unit, F-75015 Paris, France

[8] Hokkaido Univ, Grad Sch Med, Dept Microbiol & Immunol, Kita Ku, N-15,W-7, Sapporo, Hokkaido 0608638, Japan

[9] Natl Inst Hlth Sci, Div Mol Target & Gene Therapy Prod, Kawasaki Ku, 3-25-26 Tonomachi, Kawasaki, Kanagawa 2109501, Japan

[10] Yokohama City Univ, Grad Sch Med Life Sci, 1-7-29, Yokohama, Kanagawa 2300045, Japan

来源：

JOURNAL OF PHARMACOLOGICAL SCIENCES | 2022年 / 149卷 / 03期

关键词：

SARS-CoV2; Antiviral activity; Ciclesonide;

D O I：

10.1016/j.jphs.2022.04.001

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 antiCOVID-19 agents. (c) 2022 The Authors. Production and hosting by Elsevier B.V. on behalf of Japanese Pharmacological Society. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/).

引用

页码：81 / 84

页数：4

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