|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
18
|
|
pubmed:dateCreated |
2001-8-24
|
|
pubmed:abstractText |
The interaction of LFA-1 and ICAM-1 plays an important role in the cell adhesion process. On the basis of previously reported SAR and structural information on the binding of our p-arylthiocinnamide series to LFA-1, we have identified the cyclic amide (C-ring) as a site for modification. Improvement in potency and, more importantly, in the physical properties and pharmacokinetic profiles of the leading compounds resulted from this modification. One of the best compounds (11f) is also shown to reduce myocardial infarct size in rat.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Aug
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
pubmed-author:ABEG YGY,
pubmed-author:DeVriesPP,
pubmed-author:GaySS,
pubmed-author:HuthJ RJR,
pubmed-author:LUMM,
pubmed-author:LeitzaSS,
pubmed-author:LinNN,
pubmed-author:LindJ MJM,
pubmed-author:LubbersN LNL,
pubmed-author:MarshK CKC,
pubmed-author:OkasinskiG FGF,
pubmed-author:PerSS,
pubmed-author:ReillyE BEB,
pubmed-author:XieSS,
pubmed-author:von GeldernT WTW
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
30
|
|
pubmed:volume |
44
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2913-20
|
|
pubmed:dateRevised |
2003-11-14
|
|
pubmed:meshHeading |
pubmed-meshheading:11520199-Amides,
pubmed-meshheading:11520199-Animals,
pubmed-meshheading:11520199-Cardiovascular Agents,
pubmed-meshheading:11520199-Cell Adhesion,
pubmed-meshheading:11520199-Cell Line,
pubmed-meshheading:11520199-Cinnamates,
pubmed-meshheading:11520199-Intercellular Adhesion Molecule-1,
pubmed-meshheading:11520199-Lymphocyte Function-Associated Antigen-1,
pubmed-meshheading:11520199-Magnetic Resonance Spectroscopy,
pubmed-meshheading:11520199-Male,
pubmed-meshheading:11520199-Models, Molecular,
pubmed-meshheading:11520199-Myocardial Infarction,
pubmed-meshheading:11520199-Myocardium,
pubmed-meshheading:11520199-Nipecotic Acids,
pubmed-meshheading:11520199-Rats,
pubmed-meshheading:11520199-Rats, Sprague-Dawley,
pubmed-meshheading:11520199-Solubility,
pubmed-meshheading:11520199-Structure-Activity Relationship,
pubmed-meshheading:11520199-Sulfides
|
|
pubmed:year |
2001
|
|
pubmed:articleTitle |
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
|
|
pubmed:affiliation |
Department of Metabolic Disease Research, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA. zhonghua.pei@abbott.com
|
|
pubmed:publicationType |
Journal Article
|
