可阻断严重急性呼吸综合征冠状病毒2（SARS-CoV-2）RNA复制的环索奈德类似物的研发。
Development of ciclesonide analogues that block SARS-CoV-2 RNA replication.
作者信息
Tsuji Genichiro, Yonemitsu Kenzo, Ito Takahito, Yanase Yuta, Uema Masashi, Ohoka Nobumichi, Inoue Takao, Asakura Hiroshi, Demizu Yosuke
机构信息
Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
Division of Biomedical Food Research, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.
出版信息
Bioorg Med Chem Lett. 2021 Jul 1;43:128052. doi: 10.1016/j.bmcl.2021.128052. Epub 2021 Apr 20.
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.
环索奈德是一种用于治疗哮喘的吸入性皮质类固醇，目前正在进行治疗2019冠状病毒病（COVID-19）的临床试验。环索奈德的一种活性代谢物Cic2最近被报道可抑制严重急性呼吸综合征冠状病毒2（SARS-CoV-2）基因组RNA复制。在此，我们设计并合成了几种类型的环索奈德类似物。与带有羟基的Cic2相比，带有叠氮基的Cic4和带有氯基的Cic6能有效降低SARS-CoV-2病毒复制，且细胞毒性较低。这些化合物有望成为具有显著抗病毒活性的COVID-19新型治疗药物。
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