Design, synthesis, and SAR of cis-1, 2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: Exploration of 5–6 fused rings as alternative S1 moieties

K Yoshikawa, A Yokomizo, H Naito, N Haginoya…

文献索引：Yoshikawa, Kenji; Yokomizo, Aki; Naito, Hiroyuki; Haginoya, Noriyasu; Kobayashi, Shozo; Yoshino, Toshiharu; Nagata, Tsutomu; Mochizuki, Akiyoshi; Osanai, Ken; Watanabe, Kengo; Kanno, Hideyuki; Ohta, Toshiharu Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 24 p. 8206 - 8220

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被引用次数: 22

摘要

A series of cis-1, 2-diaminocyclohexane derivatives were synthesized with the aim of optimizing previously disclosed factor Xa (fXa) inhibitors. The exploration of 5–6 fused rings as alternative S1 moieties resulted in two compounds which demonstrated improved solubility and reduced food effect compared to the clinical candidate, compound A. Herein, we describe the synthesis and structure–activity relationship (SAR), together with the ...