Cyclic ether acetal platelet activating factor (PAF) receptor antagonists II: imidazo[4,5-c]pyridyl derivatives

L.Michael Wood,Mark Whittaker,David J. Timmis,Timothy M. Thompson,Lydia Saroglou,Andrew Miller,Alan H. Davidson,Mark S. Christodoulou,Karen S. Cackett,Stephen A. Bowles,Deborah S. Bebbington

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1993）

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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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