Synthesis and anti-SARS-CoV-2 activity of deuterated GS-441524 analogs
Wei Zheng1,2, Tianwen Hu3,2, Yumin Zhang4
1Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
Tetrahedron Letters
|July 18, 2022
Abstract:
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.
