Synthesis and antiviral activity of novel acyclic nucleoside analogues of 5-(1-azido-2-haloethyl)uracils

J Med Chem. 2001 Nov 22;44(24):4225-9. doi: 10.1021/jm010227k.

R Kumar ¹, N Sharma, M Nath, H A Saffran, D L Tyrrell

Affiliations

Affiliation

1 Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton T6G 2H7, Canada. [email protected]

PMID: 11708924 DOI: 10.1021/jm010227k

Abstract

We present the discovery of a novel category of 5-substituted acyclic pyrimidine nucleosides as potent Antiviral agents. A series of 1-[(2-hydroxyethoxy)methyl] (5-7), 1-[(2-hydroxy-1-(hydroxymethyl)ethoxy)methyl] (8-10), and 1-[4-hydroxy-3-(hydroxymethyl)-1-butyl] (11-13) derivatives of 5-(1-azido-2-haloethyl)uracil were synthesized and evaluated for their biological activity in Cell Culture. 1-[4-Hydroxy-3-(hydroxymethyl)-1-butyl]-5-(1-azido-2-chloroethyl)uracil (12) was the most effective Antiviral agent in the in vitro assays against DHBV (EC(50) = 0.31-1.55 microM) and HCMV (EC(50) = 3.1 microM). None of the compounds investigated showed any detectable toxicity to several stationary and proliferating host cells.

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