Bioorganic and Medicinal Chemistry p. 1487 - 1496 (2005)
Update date:2022-08-05
Topics:
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
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 site of fVIIa. Compound 1j was found to inhibit factor VIIa/TF at nanomolar concentration with improved selectivity versus fXa and thrombin and it preferentially prolonged the clotting time in the TF-dependent extrinsic pathway.
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