Novel 1H-pyrrolo[2,3-c]pyridines as acid pump antagonists (APAs)

A series of 1H-pyrrolo[2,3-c]pyridines 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 N1, C5, and C7 position of 1H-pyrrolo[2,3-c]pyridine scaffold, we have observed that compounds 14f and 14g are potent APAs with H+/K+ ATPase IC50 = 28 and 29 nM, respectively.

The synthesis of the potent acid pump antagonists 14f and 14g (IC50 = 28 and 29 nM) is reported.Figure optionsDownload as PowerPoint slide