Novel 4-substituted pyridine derivatives: Practical derivatization and biological profiles of reversible H+/K+-ATPase inhibitors

An easy method to prepare novel 4-alkoxy-, 4-alkylthio- or 4-aryloxy-5-methyl-2-[1-(hydroxymethyl)-2-(1-naphthyl)-ethyl (or -ethenyl)]pyridine derivatives having reversible inhibitory activity against H+/K+-ATPase is described. Use of a methylsulfinyl- or methylsulfonyl group as a leaving group makes it possible to effectively introduce various alkoxy or alkylthio groups into the 4-position of the pyridine ring at the final stages of synthesis. Biological profiles of the prepared compounds are briefly mentioned.