Abstract

Conformationally constrained analogues of platelet activating factor incorporating various combinations of a lipophile and a pyridine-like heterocycle via hydrogen bond acceptors such as ether and/or carbamate linked to a suitable core group such as 1,1-bis(hydroxymethyl)cycloalkane and 3,3-bis(hydroxymethyl)-oxetane, -thietane and -azetidine skeletons have been synthesized, and are shown to be powerful and selective PAF receptor antagonists.

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