Optimization of a coagulation factor VIIa inhibitor found in factor Xa inhibitor library

…, M Sugiki, M Takahashi, S Takehana, K Tashiro…

文献索引：Sagi, Kazuyuki; Fujita, Koichi; Sugiki, Masayuki; Takahashi, Mitsuo; Takehana, Shunji; Tashiro, Kazumi; Kayahara, Takashi; Yamanashi, Masahiro; Fukuda, Yumiko; Oono, Seiji; Okajima, Akiko; Iwata, Seinosuke; Shoji, Masataka; Sakurai, Kuniya Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 5 p. 1487 - 1496

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被引用次数: 19

摘要

An inhibitor of the complex of factor VIIa and tissue factor (fVIIa/TF), 2-substituted-4- amidinophenylpyruvic acid 1a, was structurally modified with the aim of increasing its potency and selectivity. The lead compound 1a was originally found in our factor Xa (fXa) inhibitor library on the basis of structural similarity of the primary binding sites of fVIIa and fXa. The design was based on computational docking studies using the extracted active ...