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Design, synthesis, and biological activity of novel factor Xa inhibitors: Improving metabolic stability by S1 and S4 ligand modification

DOI: 10.1016/j.bmc.2005.09.056

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Bioorganic and Medicinal Chemistry p. 1309 - 1330 (2006)

Update date:2022-08-05

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Authors:

Komoriya, SatoshiKomoriya, Satoshi

Kobayashi, ShozoKobayashi, Shozo

Osanai, KenOsanai, Ken

Yoshino, ToshiharuYoshino, Toshiharu

Nagata, TsutomuNagata, Tsutomu

Haginoya, NoriyasuHaginoya, Noriyasu

Nakamoto, YumiNakamoto, Yumi

Mochizuki, AkiyoshiMochizuki, Akiyoshi

Nagahara, TakayasuNagahara, Takayasu

Suzuki, MakotoSuzuki, Makoto

Shimada, TakashiShimada, Takashi

Watanabe, KengoWatanabe, Kengo

Isobe, YumikoIsobe, Yumiko

Furugoori, TaketoshiFurugoori, Taketoshi

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Article abstract of DOI:10.1016/j.bmc.2005.09.056

Serine protease factor xa (fXa) inhibitor 1 showed good ex vivo anti-fXa activity upon oral administration in rats. However, it has been revealed that 1 had low metabolic stability against human liver microsomes. To improve the metabolic stability, we att

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Full text of DOI:10.1016/j.bmc.2005.09.056

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