Development of New Non-Peptide GPIIb/IIIa Antagonists, NSL-95315 and NSL-95317, Isosteres of NSL-95300.

Abstract The synthetic and structure-activity relationship (SAR) studies of new non-peptide GPIIb/IIIa antagonists ( 1a-f and 3 ) were conducted by replacing one amide bond of NSL-95300 ( 2 ) with an ( E )-double bond or an enone group. NSL-95315 ( 1a ) and NSL-95317 ( 3 ) showed the inhibitory activity for collagen-induced human platelet aggregation with IC 50 values of 0.25 μM and 0.21 μM, respectively.