Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities

Chemical and Pharmaceutical Bulletin

Volumn 50, Issue 9, 2002, Pages 1187-1194

  Nishida, Hidemitsu ^a   Miyazaki, Yutaka ^a   Mukaihira, Takafumi ^a   Saitoh, Fumihiko ^a   Fukui, Miyuki ^a   Harada, Kousuke ^a   Itoh, Manabu ^a   Muraoka, Aki ^a   Matsusue, Tomokazu ^a   Okamoto, Atsushi ^a   Hosaka, Yoshitaka ^a   Matsumoto, Miwa ^a   Ohnishi, Shuhei ^a   Mochizuki, Hidenori ^a  

^a MOCHIDA PHARMACEUTICAL CO   (Japan)

Author keywords

1 arylsulfonyl 3 piperazinone; Factor Xa inhibitor; M55551; Optical isomer; Structure activity relationship

Indexed keywords

1 (4 PYRIDINYL) 4 PIPERIDINE CARBOXALDEHYDE; 2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; 3 (TERT BUTOXYCARBONYLAMINO) N [[1 (4 PYRIDINYL) 4 PIPERIDINYL] METHYLALANINE ETHYL ESTER; 4 (AMINOMETHYL) 1 (4 PYRIDINYL) 4 PIPERIDINEMETHANOL; 4 (AMINOMETHYL) 1 (4 PYRIDINYL) 4 PIPERIDINOL; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 1 [[4 (HYDROXYIMINOMETHYL) 1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 1 [[4 (HYDROXYMETHYL) 1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 1 [[4 HYDROXY 1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 (HYDROXYMETHYL) 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 (METHOXYMETHYL) 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXALDEHYDE 2 OXIME; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXAMIDE; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXYLIC ACID; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXYLIC ACID ETHYL ESTER; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXYLIC ACID METHYLESTER; 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINECARBOXYLIC ACID; 4 [4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXOPIPERAZINYL]METHYL 1 (4 PYRIDINYL) 4 PIPERIDINE CARBOXYLIC ACID; 4 [4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 6 OXOPIPERAZINYL]METHYL 1 (4 PYRIDINYL) 4 PIPERIDINE CARBOXYLIC ACID METHYLESTER; 6 (AMINOMETHYL) 4 [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL]PIPERAZINONE; 6 OXO 1 [[1 (4 PYRIDINYL) 4 PIPERIDINYL]METHYL] 2 PIPERAZINE CARBOXYLIC ACID ETHYL ESTER; [(4 HYDROXY 4 PIPERIDINYL)METHYL]CARBAMIC ACID 1,1 DIMETHYLETHYL ESTER; [[(4 HYDROXYMETHYL) 4 PIPERIDINYL]METHYL]CARBAMIC ACID 1,1 DIMETHYLETHYL ESTER; [[4 (HYDROXYMETHYL) 1 (1 OXIDO 4 PIPERIDINYL) 4 PIPERIDINYL]METHYL]CARBAMIC ACID 1,1 DIMETHYLETHYL ESTER; [[4 HYDROXY 1 (1 OXIDO 4 PIPERIDINYL)4 PIPERIDINYL]METHYL]CARBAMIC ACID 1,1 DIMETHYLETHYL ESTER; [N [4 [(1 ACETIMIDOYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL]ACETIC ACID; BLOOD CLOTTING FACTOR 10A INHIBITOR; M 55113; M 55551; N [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] N (2 OXOETHYL)GLYCINE ETHYL ESTER; N [(6 CHLORO 2 NAPHTHALENYL)SULFONYL] N (2,2 DIETHOXYETHYL)GLYCINE ETHYL ESTER; PIPERAZINE DERIVATIVE; THROMBIN; TRYPSIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; ARYLSULFONIC ACID DERIVATIVE; BLOOD CLOTTING FACTOR 10A; DYES, REAGENTS, INDICATORS, MARKERS AND BUFFERS; PIPERIDINE DERIVATIVE; TRYPSIN INHIBITOR;

ARTICLE; BIOLOGICAL ACTIVITY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; EVALUATION; IC 50; SUBSTITUTION REACTION; CRYSTALLIZATION; DRUG ANTAGONISM; HYDROGEN BOND; OXIDATION REDUCTION REACTION; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ARYLSULFONATES; CRYSTALLIZATION; FACTOR XA; HYDROGEN BONDING; INDICATORS AND REAGENTS; OXIDATION-REDUCTION; PIPERAZINES; PIPERIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBIN; TRYPSIN INHIBITORS;

EID: 19044367143     PISSN: 00092363     EISSN: 13475223     Source Type: Journal    
DOI: 10.1248/cpb.50.1187     Document Type: Article

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