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Studies on proton pump inhibitors. I. Synthesis of 8-[(2-benzimidazolyl)sulfinyl]-5,6,7,8-tetrahydroquinolines and related compounds.
- Source :
-
Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] 1989 Jun; Vol. 37 (6), pp. 1517-23. - Publication Year :
- 1989
-
Abstract
- Many 8-[(2-benzimidazolyl)sulfinyl]-5,6,7,8-tetrahydroquinolines were synthesized and examined for their (H+ + K+) adenosine triphosphatase ATPase-inhibitory and antisecretory activities. These sulfinyl compounds could be considered to be rigid analogues of the 2-[(2-pyridyl)methylsulfinyl]benzimidazole class of antisecretory agents. All the compounds tested were potent inhibitors of (H+ + K+)ATPase. Most of the compounds also inhibited histamine-induced gastric acid secretion in rats. Among them, 8-[(5-fluoro-2-benzimidazolyl)sulfinyl]-3-methyl-5,6,7,8-tetrahydroqu inoline (XIVm) was found to have the most potent activity. The structure-activity relationships are discussed.
- Subjects :
- Animals
Benzimidazoles chemical synthesis
Cell Survival drug effects
Chemical Phenomena
Chemistry
H(+)-K(+)-Exchanging ATPase
Male
Quinolines chemical synthesis
Rats
Rats, Inbred Strains
Structure-Activity Relationship
Adenosine Triphosphatases antagonists & inhibitors
Anti-Ulcer Agents chemical synthesis
Benzimidazoles pharmacology
Quinolines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0009-2363
- Volume :
- 37
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Chemical & pharmaceutical bulletin
- Publication Type :
- Academic Journal
- Accession number :
- 2550154
- Full Text :
- https://doi.org/10.1248/cpb.37.1517