Decarboxylase inhibition and structure-activity relationship studies with some newly synthetized benzyloxyamine and pyridylmethoxyamine derivatives
| Autor: | J. Kosary, J. Borsy, Géza Szilágyi, Zsuzsanna Huszti, E. Kasztreiner |
|---|---|
| Rok vydání: | 1973 |
| Předmět: |
Male
Monoamine Oxidase Inhibitors Time Factors Carboxy-Lyases Pyridines Swine Stereochemistry Chemical structure Guinea Pigs In Vitro Techniques Hydroxylamines Kidney Biochemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Methoxyamine Benzyl Compounds Animals Structure–activity relationship Histidine Amino Acids Lung Pharmacology Aromatic L-amino acid decarboxylase Stomach Brain Histidine decarboxylase In vitro Rats Liver chemistry Histamine H1 Antagonists Amine Oxidase (Copper-Containing) Histamine |
| Zdroj: | Biochemical Pharmacology. 22:2267-2275 |
| ISSN: | 0006-2952 |
| DOI: | 10.1016/0006-2952(73)90007-5 |
| Popis: | Decarboxylase inhibiting properties and the structure-activity relationship have been studied with a number of newly synthetized benzyloxyamines and pyridylmethoxyamines. In the case of benzyloxyamines, the 3-hydroxyl group, and in that of pyridylmethoxyamines, the position of methoxyamine group in the molecule, appear to be of special importance for inhibition of aromatic l -amino acid decarboxylase. We did not find any close relationship between specific histidine decarboxylase inhibiting effect and chemical structure. 3-Hydroxy-4-nitrobenzyloxyamine and pyridyl-3-methoxyamine were the most active compounds in these series. The former compound affected markedly both aromatic l -amino acid decarboxylase and histidine decarboxylase in vitro and in vivo and produced a significant decrease in the levels of histamine in the stomach and in the lungs. The latter compound proved to be a specific inhibitor of histidine decarboxylase and had a more pronounced effect on the tissue histamine levels than most of new and old benzyloxyamine derivatives. |
| Databáze: | OpenAIRE |
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