475504-88-2Relevant academic research and scientific papers
Cinnamylindoline derivatives: Synthesis and factor Xa (FXa) inhibitory activities
Noguchi, Tetsuji,Tanaka, Naoki,Nishimata, Toyoki,Goto, Riki,Hayakawa, Miho,Sugidachi, Atsuhiro,Ogawa, Taketoshi,Asai, Fumitoshi,Fujimoto, Koichi
, p. 1494 - 1504 (2008/12/23)
A series of cinnamylindoline derivatives were synthesized, and their factor Xa (FXa) inhibitory activities and selectivity over trypsin were evaluated. Among them, some novel derivatives showed potent FXa inhibitory activities and good selectivity over trypsin. Especially, (E)-2-{5-[1-(acetimidoyl)piperidin-4- yloxy]-2-[2-(5-amidino-2-hydroxyphenyl)ethen-1-yl]indolin-1-ylsulfonyl}acetic acid (22f) having 2-hydroxycinnamyl moiety exhibited the most potent FXa inhibitory activity in vitro. Furthermore, 22f also exhibited potent anticoagulant activities in vitro.
BENZAMIDINE DERIVATIVES
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, (2008/06/13)
Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R 1represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R 2represents a hydrogen atom, a halogen atom or an alkyl group, R 3represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R 4and R 5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R 6represents a substituted pyrrolidine group or substituted piperidine group.
