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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
1997-9-9
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pubmed:abstractText |
A new series of 2-[(2-aminobenzyl, 4-aminobenzyl, and alpha-methylbenzyl) sulfinyl]-N-(4-pyridinyl)-3-pyridinecarboxamides. was synthesized and evaluated for gastric antisecretory activities. Several of the compounds synthesized exhibited potent inhibitory activities against [14C]aminopyrine accumulation stimulated by dibutyryl cyclic AMP in isolated rabbit parietal cells and histamine-induced gastric acid secretion in pylorus-ligated rats by intraduodenal administration. In particular, the more polar diastereoisomer of 2-[(4-methoxy-alpha-methylbenzyl)sulfinyl] -N-(4-pyridinyl)-3-pyridinecarboxamide (13b) showed in vivo inhibitory activity equivalent or superior to that of omeprazole and was a more selective (H+/K+)-ATPase inhibitor than omeprazole.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0009-2363
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1177-82
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:9246752-Animals,
pubmed-meshheading:9246752-Antacids,
pubmed-meshheading:9246752-Enzyme Inhibitors,
pubmed-meshheading:9246752-Gastric Acid,
pubmed-meshheading:9246752-Gastric Mucosa,
pubmed-meshheading:9246752-H(+)-K(+)-Exchanging ATPase,
pubmed-meshheading:9246752-Male,
pubmed-meshheading:9246752-Niacinamide,
pubmed-meshheading:9246752-Parietal Cells, Gastric,
pubmed-meshheading:9246752-Pyridines,
pubmed-meshheading:9246752-Rabbits,
pubmed-meshheading:9246752-Rats,
pubmed-meshheading:9246752-Rats, Wistar,
pubmed-meshheading:9246752-Secretory Rate,
pubmed-meshheading:9246752-Structure-Activity Relationship
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pubmed:year |
1997
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pubmed:articleTitle |
Nicotinamide derivatives as a new class of gastric (H+/K+)-ATPase inhibitors. III. Synthesis and gastric antisecretory activity of 2-[(2- and 4-aminobenzyl, and alpha-methylbenzyl)sulfinyl]-N-(4-pyridinyl) -3-pyridinecarboxamides.
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pubmed:affiliation |
Discovery Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article
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