Thromboxane Synthase Inhibitors and Thromboxane A2 Receptor Antagonists: A Quantitative Structure Activity Relationships (QSARs) Analysis

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Abstract:

Thromboxane A2 (TxA2), a bioactive metabolite of the Arachidonic acid (AA), is a potent mediator of platelet aggregation, vasoconstriction and bronchoconstriction. It plays an important role in major human diseases, such as myocardial infraction, unstable angina, pregnancy-induced hypertension and preeclampsia, thrombosis and thrombotic disorders, pulmonary hypertension, asthma, septic shock, atherosclerosis, lupus nephritis, and Raynaud's phenomenon. Thus, TxA2 is a therapeutic target for many research groups. A number of TXA(2) receptor antagonists as well as thromboxane synthase inhibitors have been developed. In this research we review and evaluate new quantitative structure activity relationships of thromboxane synthase inhibitors and thromboxane receptor antagonists, using the C-QSAR program of Biobyte. Lipophicity, as Clog P is a significant physicochemical parameter for this biological response. CMR/MR molar refractivity as well as sterimol parameters seemed to be important as well Molecular Volume. Electronic effects with the exception of  Hammett's constant are not found to govern the biological activity. The derived equations will be very helpful for the design of new potent molecules.

Keywords: QSAR; lipophilicity; steric factors; thormboxane receptor antagonists; thromobxane synthase inhibitors

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986710792231978

Affiliations: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Chemistry, 54124, Thessaloniki, Greece.

Publication date: September 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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