Discovery of R-142086 as a factor Xa (FXa) inhibitor: Syntheses and structure-activity relationships of cinnamyl derivatives1,2

Chemical and Pharmaceutical Bulletin

Volumn 57, Issue 1, 2009, Pages 22-33

  Noguchi, Tetsuji ^a   Tanaka, Naoki ^a   Nishimata, Toyoki ^a   Goto, Riki ^a   Hayakawa, Miho ^a   Sugidachi, Atsuhiro ^a   Ogawa, Taketoshi ^a   Niitsu, Yoichi ^a   Asai, Fumitoshi ^a   Ishizuka, Tomoko ^a   Fujimoto, Koichi ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Ames test; Anticoagulant; Cinnamyl derivative; Factor Xa inhibitory activity; Prodrug

Indexed keywords

[N [4 [(1 ACETIMIDOYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL]ACETIC ACID METHANESULFONATE; [N [4 [1 (ACETIMIDOYL)PIPERIDIN 4 YLOXY] 3 CARBAMOYLPHENYL] N [3 (3 AMIDINOPHENYL) 2 FLUORO 2 PROPENYL]SULFAMOYL]ACETIC ACID; ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; R 142086; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTICOAGULATION; ARTICLE; DOG; DOSE RESPONSE; DRUG DOSE COMPARISON; DRUG EFFECT; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; EX VIVO STUDY; HAMSTER; LIPOPHILICITY; NONHUMAN; PROTHROMBIN TIME; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; AMIDINES; ANIMALS; ANTICOAGULANTS; ANTITHROMBIN III; CINNAMATES; CRICETINAE; DOGS; FACTOR XA; HUMANS; MALE; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES;

EID: 58849158474     PISSN: 00092363     EISSN: 13475223     Source Type: Journal    
DOI: 10.1248/cpb.57.22     Document Type: Article

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