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Tsuji, Genichiro; Nakajima, Shogo; Watashi, Koichi; Torii, Shiho; Suzuki, Rigel; Fukuhara, Takasuke; Ohoka, Nobumichi; Inoue, Takao; Demizu, Yosuke
Journal of pharmacological sciences, 07/2022, Volume: 149, Issue: 3Journal Article
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.
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