Chapter 9. Agents for the Treatment of Peptic Ulcer Disease

Molecular and Crystal Structures of 2-(2-Pyridyl)thioacetamide Derivatives and Possible Relationship with Inhibitory Activity for Gastric Acid Secretion

“…In conclusion, it was verified by QSAR analyses that the following two characteristics are important for the inhibitory activity of 2-(2-pyridyl)thioacetamide derivatives: (1) the spatial dispositions of S(9), N(10), S(7%), or O(72) andN(73) or O(73) atoms with respect to the pyridine ring; and (2) the whole molecular conformation and its chemical structure.…”

“…1 Recently, (H' + K+)-ATPase has been recognized as the acid pump involved in the terminal steps of the gastric acid secretory process, and thus (H' + K+)-ATPase inhibitors, such as omeprazole, have attracted attention.= A series of compounds having 242-pyridy1)thioacetamide as a fundamental skeleton has recently been synthesized to explore the novel antiulcer candidates which exert both potent gastric mucosal protective and antisecretory activities. Pharmacological inhibition of gastric acid has been accomplished by histamine H,-receptor antagonists and anticholinergics.…”