BASE-FUNCTIONALIZED CARBOCYCLIC NUCLEOSIDES: DESIGNSYNTHESIS AND MECHANISM OF ANTIVIRAL ACTIVITY

摘要

New carbocyclic ribonucleosides with unsaturated groups at the C-2 position of the nucleobase were designed as potential RNA antiviral compounds. The design was based on the expectation that the monophosphates of these compounds would be inhibitors of the enzyme, IMPDH. Appropriate methodologies were developed to achieve the target molecules. Results from the initial in vitro antiviral studies are mentioned. The IMPDH-associated mechanism of the antiviral activity of the most active compound is supported by enzyme inhibition studies.