Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs

• DOI: 10.1016/j.tetlet.2022.154012
• Publication Date: 2022-07-09T15:10:07Z
• Authors: Wei Zheng; Tianwen Hu; Yumin Zhang; Daibao Wei; Yuanchao Xie; Jingshan Shen
• Keywords: 0303 health sciences; 03 medical and health sciences; Article; 3. Good health

The COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is continuing to spread around the world. GS-441524 is the parent nucleoside of remdesivir which is the first drug approved for the treatment of COVID-19, and demonstrates strong activity against SARS-Cov-2 in vitro and in vivo. Herein, we reported the synthesis of a series of deuterated GS-441524 analogs, which had deuterium atoms up to five at the ribose and the nucleobase moieties. Compared to GS-441524, all the deuterated compounds showed similar inhibitory activities against SARS-CoV-2 in vitro.