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

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

文献索引：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

全文：HTML全文

被引用次数: 8

摘要

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 ...