Studies on proton pump inhibitors. II. Synthesis and antiulcer activity of 8-((2-benzimidazolyl)-sulfinylmethyl)-1,2,3,4-tetrahydroquinolines and related compounds.

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Abstract
Many 8-[(2-benzimidazolyl)sulfinylmethyl]-1, 2, 3, 4-tetrahydroquinoline derivatives were synthesized and tested for their (H+ + K+)adenosine triphosphatase (ATPase)-inhibitory and antisecretory activities against histamine-induced gastric acid secretion in rats. These sulfinyl compounds were synthesized by the oxidation of the corresponding sulfides, which were obtained from the reaction of 8-chloromethyl-1, 2, 3, 4-tetrahydroquinolines and 2-mercaptobenzimidazoles in the presence of potassium carbonate. All compounds tested were potent inhibitors of (H+ + K+)ATPase. Most of the compounds showed antisecretory activity. Among them, 8-[(2-benzimidazolyl)sulfinylmethyl]-1-ethyl-1, 2, 3, 4-tetrahydroquinoline (IXa) was found to have the most potent activity. The structure-activity relationships are discussed.

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