BASIC PHARMACOPHORE OF SOME ANTITHROMBOTIC AGENTS WITH COMBINED THROMBOXANE RECEPTOR ANTAGONIST (TXRA) THROMBOXANE SYNTHASE INHIBITOR (TXSI) ACTIVITY/

Platelet activation, causing formation of platelet aggregates, plays a major role in occlusive thrombus formation which may induce ischemic cardiovascular diseases. Thromboxane A(2) (TXA(2)) is an extremely pot ent vasoconstricting and platelet-aggregating agent so that it is impo rtant to search for a new type of thromboxane synthase inhibitor combi ned with thromboxane receptor antagonism (TxRA/TxSI) dual blocker with high potency and less side effects. On the basis of the structures of some known TxRA/TxSI dual blockers, we used 3D molecular modelling to search for pharmacophores for the dual blockers. (C) 1997 Wiley-Liss, Inc.