Stereochemical Aspects of the anti-HCMV Activity of Cytidine Nucleoside Analogues

Autor: Mansour, T. S., Cimpoia, A. R., Jin, H., Hunter, P. J., Evans, C. A., Tse, H. L. A., Gillard, J. W., Borthwick, A. D., Knight, D. J., Coates, J. A. V.
Zdroj: Antiviral Chemistry & Chemotherapy; June 1995, Vol. 6 Issue: 3 p138-142, 5p
Abstrakt: The remarkable selectivity of the β-L enantiomers of 2′,3′-dideoxycytidine analogues against the viral polymerases of HIV and HBV has stimulated our interest in targeting β-L enantiomers of anti-HCMV cytidine analogues. Indeed, Ara-C, FIAC and DMDC are cytidine analogues with β-D configuration that show significant potency as anti-HCMV agents but lack selectivity. β-L enantiomers have therefore been synthesized and evaluated together with four other nucleoside analogues, and the β-L. enantiomers were found not to be inhibitory to HCMV replication. However, the three α-L isomers, α-L-Ara-C, α-L-Xylo-C and α-L-FMAU, emerged with activity against HCMV and have provided new approaches for the treatment of viral diseases with nucleoside analogues possessing the unusual L-configuration.
Databáze: Supplemental Index