Adenosine analogues as inhibitors of P2Y12 receptor mediated platelet aggregation

Modified adenosine derivatives may lead to the development of P2Y12 antagonists that are potent, selective, and bind reversibly to the receptor. Analogues of 2′,3′-trans-styryl acetal-N6-ureido-adenosine monophosphate were prepared by modification of the 5′-position. The resulting analogues were tested for P2Y12 antagonism in a platelet aggregation assay.

Graphical abstractModified adenosine derivatives may lead to the development of P2Y12 antagonists that are potent, selective, and bind reversibly to the receptor. Analogues of 2′,3′-trans-styryl acetal-N6-ureido-adenosine monophosphate were prepared by modification of the 5′-position. The resulting analogues were tested for P2Y12 antagonism in a platelet aggregation assay. Compound 42 was found to be the most potent with an IC50 value of 40 nM.Figure optionsDownload full-size imageDownload as PowerPoint slide