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Synthesis and pharmacology of modified amidine isoxazoline glycoprotein IIb/IIIa receptor antagonists
T M Sielecki1, J Liu, S A Mousa
1The DuPont Pharmaceuticals Company, Experimental Station, PO Box 80500, Wilmington, DE 19880-0500, USA. thais.m.sielecki@dupontpharma.com
Bioorganic & Medicinal Chemistry Letters
|August 22, 2001
Abstract:
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.