Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists

Journal of Medicinal Chemistry

Volumn 52, Issue 14, 2009, Pages 4173-4191

  Hartz, Richard A ^a   Ahuja, Vijay T ^a   Arvanitis, Argyrios G ^a   Rafalski, Maria ^a   Yue, Eddy W ^a   Denhart, Derek J ^a   Schmitz, William D ^a   Ditta, Jonathan L ^a   Deskus, Jeffrey A ^a   Brenner, Allison B ^a   Hobbs, Frank W ^a   Payne, Joseph ^a   Lelas, Snjezana ^a   Li, Yu Wen ^a   Molski, Thaddeus F ^a   Mattson, Gail K ^a   Peng, Yong ^a   Wong, Harvey ^a   Grace, James E ^a   Lentz, Kimberley A ^a   Qian Cutrone, Jingfang ^a   Zhuo, Xiaoliang ^a   Shu, Yue Zhong ^a   Lodge, Nicholas J ^a   Zaczek, Robert ^a   Combs, Andrew P ^a   Olson, Richard E ^a   Bronson, Joanne J ^a   Mattson, Ronald J ^a   Macor, John E ^a   more..

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 CHLORO 1 (1 CYCLOPROPYL 2 METHOXYETHYL) 3 (4 METHOXY 2,5 DIMETHYLPHENYLAMINO)PYRAZIN 2 (1H) ONE; BENZENE DERIVATIVE; CORTICOTROPIN RELEASING FACTOR 1 RECEPTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CORTICOTROPIN RELEASING FACTOR RECEPTOR 1; N 3 PHENYLPYRAZINONE DERIVATIVE; PYRAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANXIETY DISORDER; ARTICLE; CONTROLLED STUDY; DEFENSIVE BEHAVIOR; DEPRESSION; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; IC 50; IN VIVO STUDY; MONKEY; NONHUMAN; RAT; RECEPTOR AFFINITY; RECEPTOR OCCUPANCY; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; TRANQUILIZING ACTIVITY;

ANIMALS; CELL LINE, TUMOR; HUMANS; MACACA FASCICULARIS; MALE; PYRAZINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 67650757154     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900301y     Document Type: Article

References (58)

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51. 2 receptor binding assay.
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58. LogD measurements were determined by partitioning of the compound between octanol and water at pH = 7.4.