Bioorganic and Medicinal Chemistry Letters p. 1211 - 1215 (2007)
Update date:2022-08-03
Topics:
Brescia, Marc-Raleigh
Rokosz, Laura L.
Cole, Andrew G.
Stauffer, Tara M.
Lehrach, John M.
Auld, Douglas S.
Henderson, Ian
Webb, Maria L.
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.
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Doi:10.1002/ejoc.202001080
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