Novel pyrimidines as acid pump antagonists (APAs)

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, IC50 = 52 nM.

The synthesis of the potent acid pump antagonist 7h (IC50 = 52 nM) is reported.Figure optionsDownload as PowerPoint slide