rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
4
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pubmed:dateCreated |
1988-5-10
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pubmed:abstractText |
Some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids were prepared, and their effect on copper-dependent amine oxidases (Cu-AOs) and FAD monoamine oxidases (MAOs) activities was tested. The compounds were not substrates for Cu-AO enzymes but acted as noncompetitive inhibitors. Hydrazides of pyrrol-1-ylphenylacetic acids were highly specific for plasma amine oxidase (Ki = 0.5-1 microM). In contrast, all the hydrazides were weak inhibitors of MAO activity. Incubation with the hydrazide derivatives led to irreversible inactivation of Cu-AOs. Therefore, the inhibition implied two distinct steps. The first one consisted of the rapid formation of the enzyme-inhibitor complex and was reversed by dialysis. In the second step, the complex was irreversibly transformed, probably by the formation of a Schiff base between the hydrazide and the prosthetic carbonyl group of the enzyme.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
pubmed:status |
MEDLINE
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pubmed:month |
Apr
|
pubmed:issn |
0022-2623
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pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
31
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
802-6
|
pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:3127589-Amine Oxidase (Copper-Containing),
pubmed-meshheading:3127589-Animals,
pubmed-meshheading:3127589-Brain,
pubmed-meshheading:3127589-Cattle,
pubmed-meshheading:3127589-Copper,
pubmed-meshheading:3127589-Flavin-Adenine Dinucleotide,
pubmed-meshheading:3127589-Humans,
pubmed-meshheading:3127589-Hydrazines,
pubmed-meshheading:3127589-Isoniazid,
pubmed-meshheading:3127589-Monoamine Oxidase Inhibitors,
pubmed-meshheading:3127589-Oxidoreductases Acting on CH-NH Group Donors,
pubmed-meshheading:3127589-Phenylacetates,
pubmed-meshheading:3127589-Pyrroles,
pubmed-meshheading:3127589-Rats
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pubmed:year |
1988
|
pubmed:articleTitle |
Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids.
|
pubmed:affiliation |
Istituto di Chimica Farmaceutica e Tossicologica, Università di Roma "La Sapienza", Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|