- Quinolinecarboxylic acid derivatives
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Quinolinecarboxylic acid derivatives represented by the following formula: STR1 wherein C is hydroxymethyl, methoxy, ethoxy or morpholinyl, or pharmaceutically acceptable salts thereof exhibit a potent action for stimulating a serotonin 4 receptor. The compounds exhibit an action of enhancing the gastrointestinal motor function to improve the gastrointestinal conditions such as heartburn, anorexia, bowel pain, abdominal distension, etc., accompanied by chronic gastritis, diabetes mellitus or postoperative gastroparesis, and are thus effective for the treatment of gastro-esophagal reflux, intestinal pseudo-obstruction and constipation.
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- Effect of Through-Bond Interaction on Conformation and Structure of Some N-Arylpiperidone and N-Aryltropanone Derivatives.
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Through-bond interaction (TBI) in N-aryl-4-piperidone derivatives in which the carbonyl group is modified to enhance its electron deficiency is found to stabilize the sterically disfavored axial arrangement of the aryl group, an arrangement also found in
- Krijnen, B.,Beverloo, H. B.,Verhoeven, J. W.,Reiss, C. A.,Goubitz, K.,Heijdenrijk, D.
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p. 4433 - 4440
(2007/10/02)
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- 5-(N-Arylnortropan-3-yl)- and 5-(N-Arylpiperidin-4-yl)-2,4-diaminopyrimidines. Novel Inhibitors of Dihydrofolate Reductase
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Based on a computer-assisted analysis of the three-dimensional structure of the binary complex of E.coli dihydrofolate reductase (DHFR) with methotrexate, 5-(N-arylnortropan-3-yl)- and 5-(N-arylpiperidin-4-yl)-2,4-diaminopyrimidines 2 and 4 were designed
- Maag, Hans,Locher, Rita,Daly, John J.,Kompis, Ivan
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p. 887 - 897
(2007/10/02)
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