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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
9
|
| pubmed:dateCreated |
1990-10-4
|
| pubmed:abstractText |
Several 3'-substituted cephalosporin sulfones were synthesized from 3-(hydroxymethyl)cephalosporin, which was prepared by Ti(OiPr)4 hydrolysis of the corresponding acetate. A method was also developed to prepare a 3-vinylcephalosporin. Some of these compound were found to be potent time-dependent inhibitors of human leukocyte elastase (HLE). The HLE inhibitory activity was correlated with sigma 1 and it was concluded that the potency was determined by the electron-withdrawing ability as well as the size of the substituent. A mechanism for inhibition of HLE by cephalosporin sulfones is proposed.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0022-2623
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
33
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
2529-35
|
| pubmed:dateRevised |
2008-11-21
|
| pubmed:meshHeading |
pubmed-meshheading:2391693-Cephalosporins,
pubmed-meshheading:2391693-Chemical Phenomena,
pubmed-meshheading:2391693-Chemistry,
pubmed-meshheading:2391693-Humans,
pubmed-meshheading:2391693-Leukocyte Elastase,
pubmed-meshheading:2391693-Pancreatic Elastase,
pubmed-meshheading:2391693-Structure-Activity Relationship,
pubmed-meshheading:2391693-Sulfones
|
| pubmed:year |
1990
|
| pubmed:articleTitle |
Inhibition of human leukocyte elastase. 3. Synthesis and activity of 3'-substituted cephalosporins.
|
| pubmed:affiliation |
Department of Medicinal Chemical Research, Merck Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.
|
| pubmed:publicationType |
Journal Article
|