rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
12
|
pubmed:dateCreated |
1992-7-30
|
pubmed:abstractText |
Nine simple and structurally flexible PAF antagonists were synthesized and their inhibitory effects on PAF induced platelet aggregation were measured. Compounds with PAF antagonistic activity exhibited a negative electrostatic potential generated by two trimethoxyphenyl groups (isocontour at -10 Kcal/mole) at various distances between the negative clouds. The optimal distance between the atoms generating the "cache-oreilles" system for exhibiting potent PAF antagonistic activity is estimated to be 11-13 A. In the flexible molecules studied, the dispersion of the electronic distribution is not necessarily favorable for anti-PAF activity. The data support the simple bipolarized model for the PAF receptor that has been proposed by the authors.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
0024-4201
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
26
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1167-71
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1668113-Animals,
pubmed-meshheading:1668113-Calorimetry,
pubmed-meshheading:1668113-Drug Design,
pubmed-meshheading:1668113-Electrochemistry,
pubmed-meshheading:1668113-Indicators and Reagents,
pubmed-meshheading:1668113-Magnetic Resonance Spectroscopy,
pubmed-meshheading:1668113-Molecular Conformation,
pubmed-meshheading:1668113-Molecular Structure,
pubmed-meshheading:1668113-Platelet Activating Factor,
pubmed-meshheading:1668113-Platelet Aggregation,
pubmed-meshheading:1668113-Platelet Membrane Glycoproteins,
pubmed-meshheading:1668113-Rabbits,
pubmed-meshheading:1668113-Receptors, Cell Surface,
pubmed-meshheading:1668113-Receptors, G-Protein-Coupled
|
pubmed:year |
1991
|
pubmed:articleTitle |
PAF receptor and "Cache-oreilles" effect. Simple PAF antagonists.
|
pubmed:affiliation |
Centre d'Ingéniérie des Protéines, Institut de Chimie, Liége-Sart-Tilman, Belgium.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|