1
5-substituted uridine(1, Br, CI), 5´-amino-5´-deoxyuridine conjugates of amino acid, peptide and penicillin G, 5´-monophophate uridine derivatives and 5´-monophosphate-fatty acid derivatives were chemically synthesized. Their biological activities were determined as MIC and ICie unit against various pathogenic microorganisms in vitro. 5´-amino-5´-deoxyuridine-cyclo(PheAspx23),5-iodo-5´-amino-deoxyuridine-penicillin G(26) were the most efficient; their IC? against L5178Y marine lymphoma cell was 6.5 g/m/, MIC against S. aureas (+) and E coli (-) was 6.25 g/ml. MIC of 5-bromo-2´,3´-O-isopropylideneuridine(6) against Trichophyron rubrum was 0.2 g/m/. And 5´-monophosphate derivatives are more active than simple uridine derivatives, suggesting other modified nucleoside 5´-phosphate may be worthwhile examining further as a new prodrugs.
|