Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 ((DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)

Journal of Medicinal Chemistry

Volumn 55, Issue 23, 2012, Pages 10610-10629

  Barlind, Jonas G ^a   Bauer, Udo A ^a   Birch, Alan M ^b   Birtles, Susan ^b   Buckett, Linda K ^b   Butlin, Roger J ^b   Davies, Robert D M ^b   Eriksson, Jan W ^a,c   Hammond, Clare D ^b   Hovland, Ragnar ^a   Johannesson, Petra ^a   Johansson, Magnus J ^a   Kemmitt, Paul D ^b   Lindmark, Bo T ^a   Morentin Gutierrez, Pablo ^b   Noeske, Tobias A ^a   Nordin, Andreas ^a   O'Donnell, Charles J ^b   Petersson, Annika U ^a   Redzic, Alma ^a   Turnbull, Andrew V ^b   Vinblad, Johanna ^a   more..

^a ASTRAZENECA R AND D   (Sweden)

^b ASTRAZENECA   (United Kingdom)

^c SAHLGRENSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

3,5 DIMETHYL 6 [4 [4 (1H TETRAZOL 5 YLMETHYL)CYCLOHEXYL]PHENYL]PYRAZINE 2 CARBOXAMIDE; [4 [4 (6 CARBAMOYL 3,5 DIMETHYLPYRAZIN 2 YL)PHENYL]CYCLOHEXYL]ACETIC ACID; [5' (6 CARBAMOYL 3,5 DIMETHYLPYRAZIN 2 YL) 2',3' DIHYDROSPIRO(CYCLOHEXANE 1,1' INDEN) 4 YL]ACETIC ACID; ACYLTRANSFERASE INHIBITOR; AZD 7687; DIACYLGLYCEROL; DIACYLGLYCEROL ACYLTRANSFERASE 1; DIACYLGLYCEROL ACYLTRANSFERASE 1 INHIBITOR; DRUG METABOLITE; GLUCURONIDE; PYRAZINAMIDE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG;

ACYLATION; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; ENZYME INHIBITION; EXPERIMENTAL DOG; HUMAN; HUMAN CELL; HUMAN EXPERIMENT; HUMAN TISSUE; IC 50; LIPOPHILICITY; LIVER MICROSOME METABOLISM; MOUSE; NONHUMAN; NORMAL HUMAN; PH; PLASMA PROTEIN BINDING; RAT; REACTION OPTIMIZATION; STRUCTURE ACTIVITY RELATION; TRIACYLGLYCEROL BLOOD LEVEL;

ACETATES; ANIMALS; DIACYLGLYCEROL O-ACYLTRANSFERASE; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; MAGNETIC RESONANCE SPECTROSCOPY; PYRAZINES; RATS; SOLUBILITY;

EID: 84870981166     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm301296t     Document Type: Article

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