Cyclic ether acetal platelet activating factor (PAF) receptor antagonists II: imidazo[4,5-c]pyridyl derivatives
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(1993)
Abstract
The 1H-2-methylimidazo[4,5-c]pyridyl group has been found to be the optimal heterocycle for a series of cyclic ether acetal PAF antagonists. A lead compound 8 inhibits [H-3]-PAF receptor binding to washed human platelets with an IC50 value of 15 nM, and both PAF-induced hypotension and endotoxin-induced hypotension in anaesthetised rats with ED50 values of 1.4 mug/kg i.v. and 19 mug/kg i.v. respectively.
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Key words
platelet activating factor,acetal platelet,receptor
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