Structure-activity relationships of 6-Methyl-benzo[ b ]thiophene-2- carboxylic Acid (1-{(S)-1-Benzyl-4-[4-(tetrahydropyran-4-ylmethyl)piperazin-1- yl]butylcarbamoyl}cyclopentyl)amide, potent antagonist of the neurokinin-2 receptor

Journal of Medicinal Chemistry

Volumn 53, Issue 10, 2010, Pages 4148-4165

  Fattori, Daniela ^a   Porcelloni, Marina ^a   Dandrea, Piero ^a   Catalioto, Rose Marie ^a   Ettorre, Alessandro ^a   Giuliani, Sandro ^a   Marastoni, Elena ^a   Mauro, Sandro ^a   Meini, Stefania ^a   Rossi, Cristina ^a   Altamura, Maria ^a   Maggi, Carlo A ^a  

^a Menarini Ricerche SpA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

4 (2 IODOETHYL)PIPERIDINE 1 CARBOXYLIC ACID TERT BUTYL ESTER; 4 [1 [6 METHYLBENZO[B]THIOPHENE 2 CARBOXAMIDO]CYLCOPENTANECARBOXAMIDO] 5 PHENYLPENTANOIC ACID; 4 [5 PHENYL 4 (TRITYLAMINO)PENT 2 ENYL]PIPERIDINE 1 CARBOXYLIC ACID TERT BUTYL ESTER; 4 AMINO 5 PHENYL 1 [4 TETRAHYDROPYRAN 4 YLMETHYL)PIPERAZIN 1 YL]PENTAN1 ONE DIHYDROCHLORIDE; 5 ETHOXY 5 OXO 1 PHENYLPENTAN 2 AMINIUM CHLORIDE; 6 METHYL BENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [1 BENZYL 4 (4 MORPHOLIN 4 YLMETHYPIPERIDIN 1 YL)BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYL BENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [1 BENZYL 4 [4 (TETRAHYDROPYRAN 4 YLMETHYL)PIPERAZIN 1 YL]BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYL N [1 [1 PHENYL 5 (PIPERAZIN 1 YL)PENTA 2 YLCARBAMOYL)CYCLOPENTYL]BENZO[B]THIOPHENE 2 CARBOXAMIDE; 6 METHYL N [1 [5 OXO 1 PHENYLPENTAN 2 YLCARBAMOYL]CYCLOPENTYL]BENZO[B]THIOPHENE 2 CARBOXAMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [ 1 BENZYL 4 (4 MORPHOLIN 4 YLPIPERIDIN 1 YL) 4 OXOBUTYLCARBAMOYL] CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [ 1 BENZYL 4 [4 (2 HYDROXYETHYL)PIPERIDIN 1 YL]BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [ 1 BENZYL 4 OXO 4 [4 (TETRAHYDROPYRAN 4 YL )PIPERAZIN 1 YL]BUTYLCARMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [ 2 PHENYL 1 [1 (TETRAHYDROPYRAN 4 YLMETHYL)PIPERIDIN 4 YLMETHOXYMETHYL]ETHYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [ 2 PHENYL 1 [2 [1(TETRAHYDROPYRAN 4 YLMETHYL)PIPERIDIN 4 YL]ETHOXYMETHYL]ETHYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [1 BENZYL 4 (4 ETHANESULFONYLPIPERAZIN 1 YL)BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [1 BENZYL 4 (4 FORMYLPIPERAZIN 1 YL)BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [1 BENZYL 4 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL]BUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; 6 METHYLBENZO[B]THIOPHENE 2 CARBOXYLIC ACID [1 [[ 1 BENZYL 4 [4 [METHYL(TETRAHYDROPYRAN 4 YL)AMINO]PIPERIDIN 1 YL] 4 OXOBUTYLCARBAMOYL]CYCLOPENTYL]AMIDE; [2 (1 TERT BUTOXYCARBONYLPIPERDIN 4 YL)ETHYL]TRIPHENYLPHOSPHONIUM IODIDE; BENZYL 4 [4 [TERT BUTYLCARBONYLAMINO] 5 PHENYLPENT 2 ENYL]PIPERAZINE 1 CARBOXYLATE; N [1 [5 [METHOXY(METHYL)AMINO] 5 OXO 1 PHENYLPENTAN 2 YLCARBAMOYL]CYCLOPENTYL] 6 METHYLBENZO[B]THIOPHENE 2 CARBOXAMIDE; NEUROKININ 2 RECEPTOR; NEUROKININ 2 RECEPTOR ANTAGONIST; TERT BUTYL 5 OXO 1 PHENYLPENT 3 EN 2 YLCARBAMATE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; BLADDER; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; GUINEA PIG; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; IN VITRO STUDY; IN VIVO STUDY; INTESTINE MUCOSA PERMEABILITY; MALE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; COLON; FURANS; GUINEA PIGS; HUMANS; INTESTINAL ABSORPTION; MALE; MOLECULAR CONFORMATION; MUSCLE CONTRACTION; MUSCLE, SMOOTH; PIPERAZINES; RADIOLIGAND ASSAY; RECEPTORS, NEUROKININ-2; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES; URINARY BLADDER;

EID: 77952697189     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100176s     Document Type: Article

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