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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
23
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pubmed:dateCreated |
2002-11-6
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pubmed:abstractText |
An esterase-sensitive amide prodrug 1 with a modified phenylpropionic acid linker was synthesized. The prodrug can be converted to the drug using isolated porcine esterase and human plasma. Paraoxon, an esterase inhibitor, can inhibit prodrug-to-drug conversion. The conversion of prodrug 1 was via phenol intermediate 9 followed by a lactonization reaction to give lactone 2 and the drug.
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pubmed:grant |
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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 |
Dec
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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 |
2
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3439-42
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12419379-Amides,
pubmed-meshheading:12419379-Animals,
pubmed-meshheading:12419379-Cholinesterase Inhibitors,
pubmed-meshheading:12419379-Drug Stability,
pubmed-meshheading:12419379-Esterases,
pubmed-meshheading:12419379-Humans,
pubmed-meshheading:12419379-Lactones,
pubmed-meshheading:12419379-Liver,
pubmed-meshheading:12419379-Paraoxon,
pubmed-meshheading:12419379-Phenylpropionates,
pubmed-meshheading:12419379-Prodrugs,
pubmed-meshheading:12419379-Substrate Specificity,
pubmed-meshheading:12419379-Swine,
pubmed-meshheading:12419379-Time Factors
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis and stability study of a modified phenylpropionic acid linker-based esterase-sensitive prodrug.
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pubmed:affiliation |
Department of Pharmaceutical Chemistry, The University of Kansas, Lawrence, KS 66047, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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