- Structural Factors Affecting the Basicity of ω-Pyridylalkanols, ω-Pyridylalkanamides and ω-Pyridylalkylamines
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The present paper describes the preparation by conventional methods (when not available commercially) and the pKa-determination of the α-, β- and γ-isomers of pyridylethanamide, 3-pyridylpropanamide, 4-pyridylbutanamide, 5-pyridylpentanamide, pyridylmethanol, 2-pyridylethanol, 3-pyridylpropanol, 4-pyridylbutanol, 5-pyridylpentanol, pyridylmethylamine, 2-pyridylethylamine, 3-pyridylpropylamine, 4-pyridylbutylamine, and 5-pyridylpentylamine.While a field effect accounts for many variations in pKa as a function of chain length, marked inductive effects are operative in some methyl and ethyl homologs.The pKa-decreasing influence of an intramolecular H-bond is also apparent in some lower homologs belonging to the α-series.
- Mayer, Joachim M.,Testa, Bernard
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p. 1868 - 1884
(2007/10/02)
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- 5-(HYDROXYPYRIDYLALKYL)-4-PYRIMIDONES
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The compounds are substituted 2-amino-4-pyrimidones with a 5-(hydroxypyridylalkyl) substituent which are histamine H 2-antagonists. Two specific compounds are 2-2-(3-bromo-2-pyridylmethylthio) ethylamino!-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimidone and 2-4-(3-methoxy-2-pyridyl)butylamino!-5-(2-hydroxy-4-pyridylmethyl)-4-pyrimido ne.
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- PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING H-1 AND H-2 HISTAMINE RECEPTORS
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Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N"-2-((4-methyl-5-imidazolyl)-methylthio)ethyl!guanidine. "
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