Stereoselective synthesis and biological evaluation of 3, 4-diaminocyclohexanecarboxylic acid derivatives as factor Xa inhibitors

…, S Kobayashi, S Komoriya, T Yoshino, H Kanno

文献索引：Nagata, Tsutomu; Nagamochi, Masatoshi; Kobayashi, Shozo; Komoriya, Satoshi; Yoshino, Toshiharu; Kanno, Hideyuki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 16 p. 4587 - 4592

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被引用次数: 11

摘要

There have been few reports on synthetic methods for cis-1, 2-diaminocyclohexane bearing a third ring substituent. Starting from 3-cyclohexenecarboxylic acid, we developed efficient methods for synthesizing the 3, 4-diaminocyclohexanecarboxylic acid derivatives 2–5. We also evaluated their anti-Xa and anticoagulant activities. Among the compounds, acid 2a and amide 2b exhibited the most potent in vitro anti-fXa activity, indicating that the position ...