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A series of 1H-pyrrolo[2,3-c]pyridine-7-amine derivatives were designed and synthesized based on our docking model as potassium-competitive acid blockers (P-CABs). Molecular modeling of these derivatives led us to introduce a substituent at the 1-position to access two lipophilic sites and polar residues. We identified potent P-CABs that exhibit excellent inhibitory activity in vitro and in vivo. These results indicate that the 1H-pyrrolo[2,3-c]pyridine-7-amine derivatives are promising lead compounds as P-CABs.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Molecular Modeling, Design, Synthesis, and Biological Activity of 1&lt;i&gt;H&lt;/i&gt;-Pyrrolo[2,3-&lt;i&gt;c&lt;/i&gt;]pyridine-7-amine Derivatives as Potassium-Competitive Acid Blockers