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 A₂ (TXA₂) is an extremely potent vasoconstricting and platelet-aggregating agent so that it is important to search for a new type of thromboxane synthase inhibitor combined 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. Drug Dev. Res. 39:197–200. © 1997 Wiley-Liss, Inc.