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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
1999-2-2
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pubmed:abstractText |
Kynurenine 3-hydroxylase (KYN 3-OHase) is a key enzyme in the kynurenine pathway of tryptophan degradation and its inhibition may be an effective mechanism for counteracting neuronal excitotoxic damage. We present here a new class of inhibitors derived from a structure-activity relationship (SAR) study of the benzoylalanine side-chain of 1. 2-hydroxy-4-(3,4-dichlorophenyl)-4-oxobutanoic acid (8) and 2-benzyl-4-(3,4-dichlorophenyl)-4-oxo-butanoic acid (10) emerged as the most interesting derivatives. Enantiospecific synthesis for both enantiomers of 8 and diastereomeric salt resolution for those of 10 were successfully applied.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
20
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2907-12
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:9873646-Animals,
pubmed-meshheading:9873646-Brain,
pubmed-meshheading:9873646-Enzyme Inhibitors,
pubmed-meshheading:9873646-Humans,
pubmed-meshheading:9873646-Inhibitory Concentration 50,
pubmed-meshheading:9873646-Kynurenine 3-Monooxygenase,
pubmed-meshheading:9873646-Liver,
pubmed-meshheading:9873646-Mixed Function Oxygenases,
pubmed-meshheading:9873646-Phenylbutyrates,
pubmed-meshheading:9873646-Rats,
pubmed-meshheading:9873646-Structure-Activity Relationship,
pubmed-meshheading:9873646-Tryptophan
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pubmed:year |
1998
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pubmed:articleTitle |
4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase.
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pubmed:affiliation |
Pharmacia & Upjohn, Chemistry Dept., Nerviano, Milan, Italy.
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pubmed:publicationType |
Journal Article
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