Synthesis and conformational analysis of a non-amidine factor Xa inhibitor that incorporates 5-methyl-4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine as S4 binding …

N Haginoya, S Kobayashi, S Komoriya…

文献索引：Haginoya, Noriyasu; Kobayashi, Syozo; Komoriya, Satoshi; Yoshino, Toshiharu; Suzuki, Makoto; Shimada, Takashi; Watanabe, Kengo; Hirokawa, Yumiko; Furugori, Taketoshi; Nagahara, Takayasu Journal of Medicinal Chemistry, 2004 , vol. 47, # 21 p. 5167 - 5182

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被引用次数: 46

摘要

Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N- (6-chloronaphthalen-2-yl) sulfonylpiperazine derivatives incorporating various fused-bicyclic rings containing an aliphatic amine expected to be S4 binding element. Among this series, 5- methyl-4, 5, 6, 7-tetrahydrothiazolo [5, 4-c] pyridine type 61 displayed orally potent anti-fXa ...