cis-trans-Isomerization of [E]-5-(2-bromovinyl)-2,2′-anhydrouridinein vivoin rats
- 1 January 1991
- journal article
- research article
- Published by Taylor & Francis in Xenobiotica
- Vol. 21 (3) , 359-369
- https://doi.org/10.3109/00498259109039476
Abstract
1. [E]-5-(2-bromovinyl)-2,2′-anhydrouridine ([E]BVANUR) has considerable antiviral activity against herpes simplex virus type 1 (HSV-1). 2. [E]BVANUR is not a substrate of pyrimidine nucleoside phosphorylases, but it is an inhibitor of uridine phosphorylase (Ki=450 nM). 3. [E]BVANUR (trans-isomer, parent compound) undergoes isomerization to [Z]BVANUR (cis-isomer), the only metabolite in rat, which was identified by h.p.l.c., mass spectra and n.m.r. spectroscopy. 4. Absorption of the drug from the gastrointestinal tract after oral administration is minimal. Absorption of [E]BVANUR from the abdominal cavity after i.p. administration was slow.Keywords
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