Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

…, S Kobayashi, T Nagata, A Mochizuki, M Suzuki…

文献索引：Komoriya, Satoshi; Haginoya, Noriyasu; Kobayashi, Shozo; Nagata, Tsutomu; Mochizuki, Akiyoshi; Suzuki, Masanori; Yoshino, Toshiharu; Horino, Haruhiko; Nagahara, Takayasu; Suzuki, Makoto; Isobe, Yumiko; Furugoori, Taketoshi Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 12 p. 3927 - 3954

全文：HTML全文

被引用次数: 22

摘要

Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral analysis. Modification of lead compound 7 by transformation of its N-oxide 6–6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays. The optimized compounds 73b and 75b showed sub to one digit micromolar anticoagulant activity (PTCT2). Particularly, anti-fXa ...