Thromboxane modulating agents. 2. Thromboxane receptor antagonists derived from the thromboxane synthase inhibitor dazmegrel.

The design of dual thromboxane synthase inhibitor/thromboxane receptor antagonists (e.g. 15) based on the structure of the thromboxane synthase inhibitor dazmegrel is described. More potent receptor antagonists (e.g. 16c) result from replacement of the pyridinyl subsituent with 4-fluorophenyl. Modelling suggests the existence of more than one site capable of interacting with the aryl sulfonamide of TxA2 receptor antagonists.