Title of article
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists
Author/Authors
Marc-Raleigh Brescia، نويسنده , , Laura L. Rokosz، نويسنده , , Andrew G. Cole، نويسنده , , Tara M. Stauffer، نويسنده , , John M. Lehrach، نويسنده , , Douglas S. Auld، نويسنده , , Ian Henderson، نويسنده , , Maria L. Webb، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
1211
To page
1215
Abstract
The discovery and evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin (IP) receptor antagonists is described. Analogs disclosed showed high affinity for the IP receptor in human platelet membranes with IC50 values of 0.05–0.50 μM, demonstrated functional antagonism by inhibiting cAMP production in HEL cells with IC50 values of 0.016–0.070 μM, and exhibited significant selectivity versus other prostanoid receptors.
Keywords
Prostacyclin , PGI2 , pain , inflammation , Prostanoid receptors , ECLiPS™
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797820
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