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Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists
T M Sielecki1, J Wityak, J Liu
1DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA. thais.m.sielecki@dupont.harma.com
Bioorganic & Medicinal Chemistry Letters
|April 1, 2000
Abstract:
A series of ring constrained analogues of the GPIIb/IIIa receptor antagonist XR299 (1) was investigated as potential inhibitors of glycoprotein IIb/IIIa, a platelet receptor that plays a key role in platelet aggregation and platelet adhesion. Ring size was found to have a large effect on in vitro potency. Selected compounds showed good in vitro activity, a preference for binding to activated platelets, and modest duration of action when dosed i.v. as a racemate in a canine model.