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 Ki value of 1.1 ± 0.2 nM with uridine phosphorylase from human liver. The new inhibitors are easily synthesized and are better inhibitors of human uridine phosphorylase than their uracil counterparts. Copyright © 1993 Journal of Heterocyclic Chemistry
