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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1992-3-17
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pubmed:abstractText |
A new series of sulfonic acids were synthesized and tested for their enkephalinase inhibitory activity. Among them, the most potent was N-(2-benzyl-3-mercaptopropionyl)metanilic acid 10i with an IC50 value of 0.27 nM. Several other analogues (10a,b,j,n,o,gg,hh) showed the inhibitory activity comparable to or greater than thiorphan (IC50 = 2.6 nM), a C-terminal carboxyl-containing inhibitor of enkephalinase. Thus compounds containing a C-terminal sulfo group, instead of the C-terminal carboxyl group, were found to show a remarkably high level of inhibition of enkephalinase. The analgesic activity of 10b, (S)-10b, and (R)-10b was also evaluated by the phenylbenzoquinone writhing test.
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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 |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
602-8
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:1738153-Analgesics,
pubmed-meshheading:1738153-Animals,
pubmed-meshheading:1738153-Enzyme Inhibitors,
pubmed-meshheading:1738153-Female,
pubmed-meshheading:1738153-Mice,
pubmed-meshheading:1738153-Molecular Conformation,
pubmed-meshheading:1738153-Neprilysin,
pubmed-meshheading:1738153-Rabbits,
pubmed-meshheading:1738153-Structure-Activity Relationship,
pubmed-meshheading:1738153-Sulfonic Acids
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pubmed:year |
1992
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pubmed:articleTitle |
A novel class of enkephalinase inhibitors containing a C-terminal sulfo group.
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pubmed:affiliation |
Research Laboratories, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article
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