Title of article :
Development of new non-peptide GPIIb/IIIa antagonists, NSL-95315 and NSL-95317, isosteres of NSL-95300
Author/Authors :
Tohru Asari، نويسنده , , Shigetaka Ishikawa، نويسنده , , Toshiki Sasaki، نويسنده , , Jun Katada، نويسنده , , Yoshio Hayashi، نويسنده , , Takeo Harada، نويسنده , , Mako Yano، نويسنده , , Emiko Yasuda، نويسنده , , Isao Uno، نويسنده , , Iwao Ojima، نويسنده ,
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 IC50 values of 0.25 μM and 0.21 μM, respectively.
