Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors

…, K Kawakami, A Mochizuki, T Nagata, M Suzuki…

文献索引：Yoshikawa, Kenji; Yoshino, Toshiharu; Yokomizo, Yoshihiro; Uoto, Kouichi; Naito, Hiroyuki; Kawakami, Katsuhiro; Mochizuki, Akiyoshi; Nagata, Tsutomu; Suzuki, Makoto; Kanno, Hideyuki; Takemura, Makoto; Ohta, Toshiharu Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 2133 - 2140

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被引用次数: 6

摘要

We previously reported on a series of cyclohexanediamine derivatives as highly potent factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an alternative scaffold. Ethylenediamine derivatives possessing a substituent at the C1 position in S configuration and phenylenediamine derivatives possessing a substituent at the C5 position demonstrated moderate to strong anti-fXa activity. Further SAR studies led to the ...