Discovery of N-{4-[(3-hydroxyphenyl)-3-methylpiperazin-1-yl]methyl-2- methylpropyl}-4-phenoxybenzamide analogues as selective kappa opioid receptor antagonists

Journal of Medicinal Chemistry

Volumn 56, Issue 11, 2013, Pages 4551-4567

  Kormos, Chad M ^a   Jin, Chunyang ^a   Cueva, Juan Pablo ^a   Runyon, Scott P ^a   Thomas, James B ^a   Brieaddy, Lawrence E ^a   Mascarella, S Wayne ^a   Navarro, Hernán A ^a   Gilmour, Brian P ^a   Carroll, F Ivy ^a  

^a RTI INTERNATIONAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 HYDROXY N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL] 4 (3 METHYLPHENOXY)BENZAMIDE; 3 CHLORO 4 (2 HYDROXYPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL]BENZAMIDE; 3 CHLORO N [ 1 [ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL] 4 (3 METHYLPHENOXY)BENZAMIDE; 3 HYDROXY N [ 1 [ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL] 4 (3 METHYLPHENOXY)BENZAMIDE; 4 (2 FLUOROPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL]BENZAMIDE; 4 (2 HYDROXY 3 METHYLPHENOXY) N [ 1 [ 4 (3 HYDROXYPHENYL) PHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL]BENZAMIDE; 4 (2 HYDROXY 5 METHYLPHENOXY) N [ 1 [ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL]BENZAMIDE; 4 (2 HYDROXYPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL] 3 METHOXYBENZAMIDE; 4 (3 BROMOPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL]BENZAMIDE; 4 (3 CHLOROPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL]BENZAMIDE; 4 (3,5 DIMETHYLPHENOXY) N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL] 2 METHYLPROPYL]BENZAMIDE; BENZAMIDE DERIVATIVE; KAPPA OPIATE RECEPTOR ANTAGONIST; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 3 METHYL 4 PHENOXYBENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (3 FLUOROPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (3 HYDROXYPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (3 METHOXYPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (3 METHYLPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (4 HYDROXYPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (4 METHOXYPHENOXY)BENZAMIDE; N 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (4 METHYLPHENOXY)BENZAMIDE; N 1 [[4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (2 HYDROXYPHENOXY)BENZAMIDE; N 1 [[4(3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL 4 (2 METHOXYPHENOXY)BENZAMIDE; N [ 1 [ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL] 3 METHOXY 4 (3 METHYLPHENOXY)BENZAMIDE; N [ 1 [ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] 3 METHYLBUTAN 2 YL] 3 METHYL 4 (3 METHYLPHENOXY)BENZAMIDE; N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL] 2 METHOXY 4 (3 METHYLPHENOXY) BENZAMIDE; N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL] 2 METHYL 4 (3 METHYLPHENOXY)BENZAMIDE; N [ 1 [[ 4 (3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL] METHYL] 2 METHYLPROPYL] 4 [3 (TRIFLUOROMETHYL)PHENOXY]BENZAMIDE; N [4 [(3 HYDROXYPHENYL) 3 METHYLPIPERAZIN 1 YL]METHYL 2 METHYLPROPYL] 4 PHENOXYBENZAMIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; BINDING ASSAY; DRUG ACTIVITY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; IN VITRO STUDY;

ANIMALS; BENZAMIDES; CHO CELLS; CRICETINAE; CRICETULUS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; MOLECULAR DOCKING SIMULATION; PIPERAZINES; RADIOLIGAND ASSAY; RECEPTORS, OPIOID, DELTA; RECEPTORS, OPIOID, KAPPA; RECEPTORS, OPIOID, MU; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84879039263     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400275h     Document Type: Article

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