Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitors III. Effect of Ring Opening of Piperazinone Moiety on Inhibition

Hidemitsu Nishida; Yutaka Miyazaki; Takafumi Mukaihira; Hiroyasu Shimada; Kazuhiro Suzuki; Fumihiko Saitoh; Masashi Mizuno; Tomokazu Matsusue; Atsushi Okamoto; Yoshitaka Hosaka; Miwa Matsumoto; Shuhei Ohnishi; Hidenori Mochizuki

doi:10.1248/cpb.52.459

Notes

Synthesis and Evaluation of 1-Arylsulfonyl-3-piperazinone Derivatives as Factor Xa Inhibitors III.
Effect of Ring Opening of Piperazinone Moiety on Inhibition

Hidemitsu Nishida, Yutaka Miyazaki, Takafumi Mukaihira, Hiroyasu Shimada, Kazuhiro Suzuki, Fumihiko Saitoh, Masashi Mizuno, Tomokazu Matsusue, Atsushi Okamoto, Yoshitaka Hosaka, Miwa Matsumoto, Shuhei Ohnishi, Hidenori Mochizuki

著者情報

キーワード: factor Xa inhibitor, 1-arylsulfonyl-3-piperazinone, M55551, structure–activity relationship

ジャーナルフリー

2004 年 52 巻 4 号 p. 459-462

DOI https://doi.org/10.1248/cpb.52.459

詳細

抄録

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.

責任著者(Corresponding author)

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