Abstract |
A series of 4-substituted 8-[(2-benzimidazolyl)sulfinylmethyl]-1,2,3,4-tetrahydroquinolin es was synthesized and examined for their (H+ + K+) adenosine triphosphatase ( ATPase)-inhibitory and antisecretory activities against histamine-induced gastric acid secretion in rats. Many compounds tested were potent inhibitors of (H+ + K+) ATPase. Most compounds showed antisecretory activity. The antiulcer activity against water-immersion stress-induced gastric ulcer, aspirin-induced gastric ulcer and gastric necrosis induced by hydrochloric acid also were tested in the rat. Some of these compounds, in particular, 4-(N-allyl-N-methylamino)-1-ethyl-8-[(5-fluoro-6-methoxy-2-benzimidazoly l) sulfinylmethyl]-1-ethyl-1,2,3,4- tetrahydroquinoline (XVIIx) were found to have potent activity. The structure-activity relationships are discussed.
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Authors | M Uchida, M Chihiro, S Morita, H Yamashita, K Yamasaki, T Kanbe, Y Yabuuchi, K Nakagawa |
Journal | Chemical & pharmaceutical bulletin
(Chem Pharm Bull (Tokyo))
Vol. 38
Issue 6
Pg. 1575-86
(Jun 1990)
ISSN: 0009-2363 [Print] Japan |
PMID | 2170036
(Publication Type: Journal Article)
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Chemical References |
- Anti-Ulcer Agents
- Benzimidazoles
- Quinolines
- Sulfides
- Adenosine Triphosphatases
- H(+)-K(+)-Exchanging ATPase
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Topics |
- Adenosine Triphosphatases
(antagonists & inhibitors)
- Animals
- Anti-Ulcer Agents
(chemical synthesis)
- Benzimidazoles
(chemical synthesis, pharmacology)
- Chemical Phenomena
- Chemistry
- H(+)-K(+)-Exchanging ATPase
- Male
- Quinolines
(chemical synthesis, pharmacology)
- Rats
- Rats, Inbred Strains
- Sulfides
(chemical synthesis, pharmacology)
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