Author/Authors :
Thais M. Sielecki، نويسنده , , John Wityak، نويسنده , , Jie Liu، نويسنده , , Shaker A. Mousa، نويسنده , , Martin Thoolen، نويسنده , , Ruth R. Wexler، نويسنده , , Richard E. Olson، نويسنده ,
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 iv as a racemate in a canine model.
