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
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
Journal title :
Bioorganic & Medicinal Chemistry Letters
