Uridine phosphorylase inhibitors: Chemical modification of benzyloxybenzyl-barbituric acid and its effects on UrdPase inhibition

Academic Article

Abstract

  • 5-(o-Benzyloxy)benzylbarbituric acid (6) and 5-(p- benzyloxy)benzylbarbituric acid (7) were prepared and their inhibitory activities compared to 5-(m-benzyloxy)-benzylbarbituric acid (BBB) a known, potent inhibitor of uridine phosphorylase (UrdPase). Compounds 6 and 7 were 18-fold and 51-fold less active, respectively, than BBB in inhibiting UrdPase. These data provide solid evidence that the 5-benzylbarbituric acids possessing meta substituents are the most active inhibitors. In addition, 2- thioBBB (11) was synthesized and it was shown to be as active an inhibitor as BBB.
  • Digital Object Identifier (doi)

    Author List

  • Guerin DJ; Mazeas D; Musale MS; Naguib FNM; Al Safarjalani ON; El Kouni MH; Panzica RP
  • Start Page

  • 1477
  • End Page

  • 1480
  • Volume

  • 9
  • Issue

  • 11