title: Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa.
abstract: A series of benzimidazole derivatives with the side chain on the nitrogen atom oriented to the prime site of factor Xa (FXa) were designed and synthesized. Compounds with substituted aminocarbonylmethyl groups as the side chain showed potent FXa inhibitory activity. Compounds 1 and 2 exhibited most potent inhibitory activity and were effective as anticoagulants in a DIC model.
authors.affiliation: Central Pharmaceutical Research Institute, Japan Tobacco Inc, 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Ueno
authors.forename: Susumu
authors.initials: S
authors.lastname: Katoh
authors.forename: Katsuyuki
authors.initials: K
authors.lastname: Yokota
authors.forename: Jun-ichi
authors.initials: J
authors.lastname: Hoshi
authors.forename: Mikio
authors.initials: M
authors.lastname: Hayashi
authors.forename: Itsuo
authors.initials: I
authors.lastname: Uchida
authors.forename: Kazuo
authors.initials: K
authors.lastname: Aisaka
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Hase
authors.forename: Hidetsura
authors.initials: H
authors.lastname: Cho
mesh_terms: D001562:Benzimidazoles / Q000737:chemistry*; D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors