Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition

…, M Mizuno, T Matsusue, A Okamoto, Y Hosaka…

Index: Nishida, Hidemitsu; Miyazaki, Yutaka; Mukaihira, Takafumi; Shimada, Hiroyasu; Suzuki, Kazuhiro; Saitoh, Fumihiko; Mizuno, Masashi; Matsusue, Tomokazu; Okamoto, Atsushi; Hosaka, Yoshitaka; Matsumoto, Miwa; Ohnishi, Shuhei; Mochizuki, Hidenori Chemical and Pharmaceutical Bulletin, 2004 , vol. 52, # 4 p. 459 - 462

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Citation Number: 5

Abstract

Compounds containing an ethylenediamine structure in place of the piperazine ring of M55113 (1) and M55551 (2) were synthesized to investigate the effects of a piperazine moiety and evaluated for activity as factor Xa (FXa) inhibitors. Most such compounds, however, exhibited lower activity (1/10—1/100) than that of M55113 and M55551 as FXa inhibitors.