Design, synthesis, and structure–activity relationships of potent GPIIb/IIIa antagonists: discovery of FK419

T Yamanaka, M Ohkubo, S Kuroda, H Nakamura…

Index: Yamanaka, Toshio; Ohkubo, Mitsuru; Kuroda, Satoru; Nakamura, Hideko; Takahashi, Fumie; Aoki, Toshiaki; Mihara, Kayoko; Seki, Jiro; Kato, Masayuki Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 13 p. 4343 - 4352

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Citation Number: 8

Abstract

The discovery of the non-peptide antiplatelet injectable agent FK419 is reported. Based on the β-turn structure of RGD peptide sequences in the α chain of fibrinogen, which binds the glycoprotein IIb/IIIa (GPIIb/IIIa) on the surface of platelets to induce platelet aggregation, the prototype 2 was designed. After further substituent effects were investigated at the α-position of the carboxylic acid in 2, we enhanced platelet aggregation inhibition, and discovered ...

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