Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition.
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.
Nishida
Hidemitsu
H
Discovery Research Center, Mochida Pharmaceutical Co., Ltd, Gotemba, Shizuoka, Japan. hnishida@michida.co.jp
Miyazaki
Yutaka
Y
Mukaihira
Takafumi
T
Shimada
Hiroyasu
H
Suzuki
Kazuhiro
K
Saitoh
Fumihiko
F
Mizuno
Masashi
M
Matsusue
Tomokazu
T
Okamoto
Atsushi
A
Hosaka
Yoshitaka
Y
Matsumoto
Miwa
M
Ohnishi
Shuhei
S
Mochizuki
Hidenori
H
D065427:Factor Xa Inhibitors; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D065427:Factor Xa Inhibitors; D007202:Indicators and Reagents; C493032:M55113; C493033:M55551; D010879:Piperazines