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Synthesis of a new class of uridine phosphorylase inhibitors
Author(s) -
Levesque Diane L.,
Wang EngChi,
Wei DauChang,
Tzeng CherngChyi,
Panzica Raymond P.,
Naguib Fardos N. M.,
El Kouni Mahmoud H.
Publication year - 1993
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570300537
Subject(s) - chemistry , uridine , glycogen phosphorylase , thymidine phosphorylase , uracil , biochemistry , enzyme , stereochemistry , nucleotide salvage , rna , nucleotide , dna , gene
A new series of potent uridine phosphorylase inhibitors have been prepared from barbituric acid. Among them, 1‐[(2‐hydroxyethoxy)methyl]‐5‐)( m‐ ‐benzyloxy)benzylbarbituric acid ( 37 , BBBA) is the most promising having a K i value of 1.1 ± 0.2 n M with uridine phosphorylase from human liver. The new inhibitors are easily synthesized and are better inhibitors of human uridine phosphorylase than their uracil counterparts.