title: Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition.
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.
authors.affiliation: Discovery Research Center, Mochida Pharmaceutical Co., Ltd, Gotemba, Shizuoka, Japan. hnishida@michida.co.jp
authors.forename: Hidemitsu
authors.initials: H
authors.lastname: Nishida
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Miyazaki
authors.forename: Takafumi
authors.initials: T
authors.lastname: Mukaihira
authors.forename: Hiroyasu
authors.initials: H
authors.lastname: Shimada
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Suzuki
authors.forename: Fumihiko
authors.initials: F
authors.lastname: Saitoh
authors.forename: Masashi
authors.initials: M
authors.lastname: Mizuno
authors.forename: Tomokazu
authors.initials: T
authors.lastname: Matsusue
authors.forename: Atsushi
authors.initials: A
authors.lastname: Okamoto
authors.forename: Yoshitaka
authors.initials: Y
authors.lastname: Hosaka
authors.forename: Miwa
authors.initials: M
authors.lastname: Matsumoto
authors.forename: Shuhei
authors.initials: S
authors.lastname: Ohnishi
authors.forename: Hidenori
authors.initials: H
authors.lastname: Mochizuki
mesh_terms: 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
chemical_list: D065427:Factor Xa Inhibitors; D007202:Indicators and Reagents; C493032:M55113; C493033:M55551; D010879:Piperazines