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 α-methylbenzyl)sulfinyl]-N-(4-pyridinyl)-3-pyridinecarboxamides

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概要

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• A new series of 2-[(2-aminobenzyl, 4-aminobenzyl, and α-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 [^<14>C]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. Inparticular, the more polar diastereoisomer of 2-[(4-methoxy-α-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.

• 公益社団法人日本薬学会の論文
• 1997-07-15

著者

• Nakamura Katsuya

  Medicinal Chemistry Research Laboratories Fujisawa Pharmaceutical Co. Ltd.

• Nakamura K

  Department Of Pharmacology School Of Pharmacy And Pharmaceutical Sciences Mukogawa Women's Univ

• Nakamura Kazufumi

  Faculty Of Pharmaceutical Sciences Kyushu University

• Nakamura Katsuji

  Tsukuba Research Laboratories Eisai Co. Ltd.

• Tada Keiko

  Discovery Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• Seto Yasuhiro

  Discovery Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• TERAUCHI Hideo

  Discovery Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• TANITAME Akihiko

  Discovery Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• NAKAMURA Keiji

  Discovery Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• NISHIKAWA yoshinori

  Discovery Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

• Terauchi H

  Chemistry Research Laboratories Dainippon Pharmaceutical Co. Ltd.:pharmaceutical Research & Tech

• Tanitame A

  Discovery Research Laboratories Dainippon Pharmaceutical Co. Ltd.

• Nishikawa Y

  Dainippon Phaceutical Co. Ltd. Osaka Jpn

• Nishikawa Yoshinori

  Discovery Research Laboratories Dainippon Pharmaceutical Co. Ltd.

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