Novel pyrimidines as acid pump antagonists (APAs)

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5735-8. doi: 10.1016/j.bmcl.2010.08.007. Epub 2010 Aug 6.

Abstract

A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a potent APA with H(+)/K(+) ATPase, IC(50) = 52 nM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Gastric Mucosa / enzymology
  • H(+)-K(+)-Exchanging ATPase / metabolism
  • Isoquinolines / chemical synthesis
  • Isoquinolines / chemistry*
  • Isoquinolines / pharmacology
  • Kinetics
  • Proton Pump Inhibitors*
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship
  • Swine

Substances

  • Enzyme Inhibitors
  • Isoquinolines
  • Proton Pump Inhibitors
  • Pyrimidines
  • H(+)-K(+)-Exchanging ATPase
  • pyrimidine