학술논문

Synthesis of 4′-Substituted Carbocyclic Uracil Derivatives and Their Monophosphate Prodrugs as Potential Antiviral Agents
Document Type
article
Source
Viruses, Vol 15, Iss 2, p 544 (2023)
Subject
antivirals
prodrugs
carbocyclic nucleosides
viral polymerase
SARS-CoV-2
influenza virus
Microbiology
QR1-502
Language
English
ISSN
1999-4915
Abstract
Over the past decades, both 4′-modified nucleoside and carbocyclic nucleoside analogs have been under the spotlight as several compounds from either family showed anti-HIV, HCV, RSV or SARS-CoV-2 activity. Herein, we designed compounds combining these two features and report the synthesis of a series of novel 4′-substituted carbocyclic uracil derivatives along with their corresponding monophosphate prodrugs. These compounds were successfully prepared in 19 to 22 steps from the commercially available (-)-Vince lactam and were evaluated against a panel of RNA viruses including SARS-CoV-2, influenza A/B viruses and norovirus.