5-Substituted 1H-pyrrolo[3,2-b]pyridines as inhibitors of gastric acid secretion

A series of novel 1H-pyrrolo[3,2-b]pyridines was prepared relying on a copper iodide catalyzed cyclization of 2-prop-1-ynylpyridin-3-amines. A structure–activity relationship was established focusing on the influence of the substitution pattern in position 1, 3, and 5 of the heterocycle on anti-secretory activity, lipophilicity, and pKa value. Some of the compounds proved to be potent inhibitors of the gastric acid pump.

A new series of 1H-pyrrolo[3,2-b]pyridines was prepared by copper(I) iodide mediated cyclization of 2-prop-1-ynyl-pyridin-3-amines and their inhibiting effect on the gastric proton pump enzyme (H+/K+ ATPase) was assessed.Figure optionsDownload as PowerPoint slide