Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4- carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 5, 1999, Pages 765-770

  Luthin, David R ^a   Rabinovich, Aleksandr K ^a   Bhumralkar, Dilip R ^a   Youngblood, Kenna L ^a   Bychowski, Richard A ^a   Dhanoa, Daljit S ^a   John M, May ^a  

^a AGOURON PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; CORTICOTROPIN RELEASING FACTOR; CORTICOTROPIN RELEASING FACTOR ANTAGONIST; CYCLIC AMP; FORSKOLIN; GUANINE NUCLEOTIDE BINDING PROTEIN; IODINE 125; OXO 7H BENZO[E]PYRIMIDINE 4 CARBOXYLIC ACID DERIVATIVE; PROOPIOMELANOCORTIN; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CORTICOTROPIN RELEASE; DOSE RESPONSE; DRUG ACTIVITY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HORMONAL REGULATION; HYPOPHYSIS; LIGAND BINDING; NEUROPATHOLOGY; NONHUMAN; RAT; REACTION ANALYSIS; RECEPTOR AFFINITY; RECEPTOR INTRINSIC ACTIVITY;

ADRENOCORTICOTROPIC HORMONE; ANIMALS; CARBOXYLIC ACIDS; CELLS, CULTURED; CYCLIC AMP; HUMANS; MALE; PITUITARY GLAND; QUINAZOLINES; RATS; RECEPTORS, CORTICOTROPIN-RELEASING HORMONE; TRANSFECTION;

ANIMALIA;

EID: 0033535367     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00075-X     Document Type: Article

References (9)

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6. 6) δ 12.05 (s, 1H), 11.66 (d, J = 8.4 Hz, 1H), 10.88 (s, 1H), 9.12 (s, 1H), 8.89 (d, J = 7.7 Hz, 1H), 8.40 (d, J = 7.7 Hz, 1H), 7.98 (brs, 2H), 7.90-7.95 (m, 1H), 7.82-7.87 (m, 1H), 4.00-4.09 (m, 1H), 3.34-3.42 (m, 1H), 3.10-3.26 (m, 2H), 2.18-2.27 (m, 1H), 1.98-2.10 (m, 3H), 1.73-1.90 (m, 4H), 1.30-1.70 (m, 8H); APCIMS m/z 483 (M+1).
7. 2 dopamine, which was in a final volume of 2 mL.
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