170725-96-9Relevant articles and documents
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists
Wityak, John,Sielecki, Thais M.,Pinto, Donald J.,Emmett, George,Sze, Jean Y.,Liu, Jie,Tobin, A. Ewa,Wang, Shuaige,Jiang, Biao,Ma, Philip,Mousa, Shaker A.,Wexler, Ruth R.,Olson, Richard E.
, p. 50 - 60 (2007/10/03)
Using the isoxazoline as a common structural feature, three series of glycoprotein IIb/IIIa receptor antagonists were evaluated, culminating in the discovery of XR299 (30). In an in vitro assay of platelet inhibition, XR299 had an IC50 of 0.24 μM and was a potent antiplatelet agent when dosed intravenously in a canine model. It was shown through X-ray studies of the cinchonidine salt 49 that the receptor required the 5(R)-stereochemistry for high potency. The ethyl ester prodrug of XR299, XR300 (29), was orally active in the dog.
