| Synthetic study of 2-[(6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9- yl)-sulfinyl]-1H-benzimidazole analogs and their biological properties as novel proton pump inhibitors. | |
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MedLine Citation:
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PMID: 7774025 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A series of 2-[(cycloalka[b]pyridinyl)sulfinyl]-1H-benzimidazoles (11) was synthesized and tested for antisecretory activity against pentagastrin-induced gastric acid secretion in rats. A novel benzimidazole derivative containing a cyclohepta[b]pyridine moiety was found to be the most potent among the congeners, which included five- to eight-membered cycloalka[b]pyridine ring systems. Some 2-[(6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl)sulfinyl]-1H- benzimidazole analogs (14) with various substituents on the aromatic rings showed superior properties to omeprazole (1) in biological examinations in vivo. A diastereoisomer, TY-11345 (28Ba), was selected as a promising agent for further evaluation. |
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Authors:
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S Yamada; T Goto; T Yamaguchi; K Aihara; K Kogi; S Narita |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Chemical & pharmaceutical bulletin Volume: 43 ISSN: 0009-2363 ISO Abbreviation: Chem. Pharm. Bull. Publication Date: 1995 Mar |
Date Detail:
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Created Date: 1995-07-07 Completed Date: 1995-07-07 Revised Date: 2008-11-21 |
Medline Journal Info:
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Nlm Unique ID: 0377775 Medline TA: Chem Pharm Bull (Tokyo) Country: JAPAN |
Other Details:
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Languages: eng Pagination: 421-31 Citation Subset: IM |
Affiliation:
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Fukushima Research Laboratories, Toa Eiyo Ltd., Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Ulcer Agents / chemical synthesis, chemistry, pharmacology Benzimidazoles / chemical synthesis*, chemistry, pharmacology* Chemistry, Physical H(+)-K(+)-Exchanging ATPase / antagonists & inhibitors Intestinal Mucosa / drug effects, secretion Magnetic Resonance Spectroscopy Male Physicochemical Phenomena Proton Pumps / antagonists & inhibitors* Rabbits Rats Rats, Sprague-Dawley Stereoisomerism Structure-Activity Relationship |
| Chemical | |
Reg. No./Substance:
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0/Anti-Ulcer Agents; 0/Benzimidazoles; 0/Proton Pumps; EC 3.6.1.10/H(+)-K(+)-Exchanging ATPase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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