Discovery of a novel small molecule agonist scaffold for the APJ receptor

Bioorganic and Medicinal Chemistry

Volumn 24, Issue 16, 2016, Pages 3758-3770

  Narayanan, Sanju ^a   Maitra, Rangan ^a   Deschamps, Jeffery R ^b   Bortoff, Katherine ^a   Thomas, James B ^a   Zhang, Yanyan ^a   Warner, Keith ^a   Vasukuttan, Vineetha ^a   Decker, Ann ^a   Runyon, Scott P ^a  

^a RTI INTERNATIONAL   (United States)

^b NAVAL RESEARCH LABORATORY   (United States)

Author keywords

AGTRL1; Apelin; APJ small molecule agonist; APLNR; Pyrazole

Indexed keywords

1 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]CYCLOHEXANECARBOXYLIC ACID; 2 CYCLOHEXYL 2 [1 (4 FLUOROPHENYL) 5 (2 HYDROXY 6 METHOXYPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]ACETIC ACID; 2 CYCLOHEXYL 2 [1 (4 FLUOROPHENYL) 5 METHYL 1H PYRAZOLE 3 CARBOXAMIDO]ACETIC ACID; 2 CYCLOHEXYL 2 [1 (4 FLUOROPHENYL) 5 PHENYL 1H PYRAZOLE 3 CARBOXAMIDO]ACETIC ACID; 2 CYCLOHEXYL 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]ACETIC ACID; 2 [2 CYCLOHEXYL 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]ACETAMIDO]ACETIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 2 PHENYLACETIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 3 METHYLBUTANOIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 4 METHYLHEXANOIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 4 METHYLPENTANOIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]ADAMANTANE 2 CARBOXYLIC ACID; 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]BENZOIC ACID; 3 CYCLOHEXYL 3 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]PROPANOIC ACID; 3 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 5 PHENYLPENTANOIC ACID; 4 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]CYCLOHEXANECARBOXYLIC ACID; 5 AMINO 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO] 5 OXOPENTANOIC ACID; 5 CYCLOHEXYL 3 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]PENTANOIC ACID; 6 AMINO 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]HEXANOIC ACID TRIFLUOROACETATE; 6 [(TERT BUTOXYCARBONYL)AMINO] 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]HEXANOIC ACID; APELIN RECEPTOR; CARBOXYLIC ACID; METHYL 2 [2 CYCLOHEXYL 2 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]ACETAMIDO]ACETATE; METHYL 5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXYLATE; MOLECULAR SCAFFOLD; N (2 AMINO 1 CYCLOHEXYL 2 OXOETHYL) 5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE; N [1 CYCLOHEXYL 2 (DIMETHYLAMINO) 2 OXOETHYL] 5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE; N [1 CYCLOHEXYL 2 (HYDROXYAMINO) 2 OXOETHYL] 5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE; N [2 (BENZYLAMINO) 1 CYCLOHEXYL 2 OXOETHYL] 5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDE; TERT BUTYL 5 CYCLOHEXYL 3 [5 (2,6 DIMETHOXYPHENYL) 1 (4 FLUOROPHENYL) 1H PYRAZOLE 3 CARBOXAMIDO]PENTANOATE; UNCLASSIFIED DRUG; UNINDEXED DRUG; APLNR PROTEIN, HUMAN; G PROTEIN COUPLED RECEPTOR; MOLECULAR LIBRARY;

ARTICLE; BINDING AFFINITY; CALCIUM MOBILIZATION; EC50; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION; AGONISTS; ANIMAL; CELL LINE; DRUG DEVELOPMENT; ELECTROSPRAY MASS SPECTROMETRY; HUMAN; MOLECULAR LIBRARY; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; X RAY CRYSTALLOGRAPHY;

ANIMALS; CELL LINE; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; HUMANS; PROTON MAGNETIC RESONANCE SPECTROSCOPY; RATS; RECEPTORS, G-PROTEIN-COUPLED; SMALL MOLECULE LIBRARIES; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84978249333     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2016.06.018     Document Type: Article

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