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Current Medicinal Chemistry

Eiditor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

New Developments on Thromboxane and Prostacyclin Modulators Part I: Thromboxane Modulators

Author(s): Jean-Michel Dogne, Xavier de Leval, Julien Hanson, Michel Frederich, Bernard Lambermont, Alexandre Ghuysen, Angela Casini, Bernard Masereel, Ke-He Ruan, Bernard Pirotte and Philippe Kolh

Volume 11 , Issue 10 , 2004

Page: [1223 - 1241] Pages: 19

DOI: 10.2174/0929867043365260

Price: $58

Abstract

The pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases can be related to arachidonic acid (AA) metabolites. One of these bioactive metabolites of particular importance is thromboxane A2 (TXA2). It is produced by the action of thromboxane synthase on the prostaglandin endoperoxide H2 (PGH2), which results from the enzymatic degradation of AA by the cyclooxygenases. TXA2 is a potent inducer of platelet aggregation, vasoconstriction and bronchoconstriction. It is involved in a series of major pathophysiological states such as asthma, myocardial ischemia, pulmonary hypertension, and thromboembolic disorders. Therefore, TXA2 receptor antagonists, thromboxane synthase inhibitors and drugs combining both properties have been developed by several pharmaceutical companies since the early 1980s. Several compounds have been launched on the market and others are under clinical evaluation. Moreover, the recent literature reported the interest of thromboxane modulators, which combine another pharmacological activity such as, platelet activating factor antagonism, angiotensin II antagonism, or 5-lipoxygenase inhibition. In this review, we will propose a description of the recently described thromboxane modulators of major interest from both a pharmacological and a chemical point of view.

Keywords: thromboxane a2, arachidonic acid, thromboxane synthase, prostanoids, thromboxane receptor antagonist, thromboxane synthase inhibitor


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