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Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition |
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| Authors: | 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 |
| Affiliation: | Discovery Research Center, Mochida Pharmaceutical Co., Ltd, Gotemba, Shizuoka, Japan. hnishida@michida.co.jp |
| 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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