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

Author information

Hidemitsu Nishida
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Yutaka Miyazaki
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Takafumi Mukaihira
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Hiroyasu Shimada
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Kazuhiro Suzuki
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Fumihiko Saitoh
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Masashi Mizuno
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Tomokazu Matsusue
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Atsushi Okamoto
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Yoshitaka Hosaka
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Miwa Matsumoto
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Shuhei Ohnishi
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
Hidenori Mochizuki
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.

Keywords: factor Xa inhibitor, 1-arylsulfonyl-3-piperazinone, M55551, structure–activity relationship

JOURNAL FREE ACCESS

2004 Volume 52 Issue 4 Pages 459-462

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

Details

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.

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