Synthesis and pharmacology of modified amidine isoxazoline glycoprotein IIb/IIIa receptor antagonists.

Bioorg Med Chem Lett

The DuPont Pharmaceuticals Company, Experimental Station, PO Box 80500, Wilmington, DE 19880-0500, USA.

Published: August 2001

Selective antagonism of the platelet GPIIb/IIIa receptor represents an attractive mechanism for the prevention and treatment of a number of thrombotic disease states. The antiplatelet activity of the oral GPIIb/IIIa receptor antagonists DMP 754 and DMP 802 have been disclosed. In this paper, the synthesis and biological evaluation of a series of potent N-substituted benzamidine isoxazolines are explored. The effect of benzamidine substitution on the duration of antiplatelet efficacy in dog is presented.

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http://dx.doi.org/10.1016/s0960-894x(01)00406-1DOI Listing

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