Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 15, 2009, Pages 4070-4074

  Koltun, Dmitry O ^a   Zilbershtein, Timur M ^b   Migulin, Vasily A ^c   Vasilevich, Natalya I ^b   Parkhill, Eric Q ^a   Glushkov, Andrei I ^b   McGregor, Malcolm J ^d   Brunn, Sandra A ^a   Chu, Nancy ^a   Hao, Jia ^a   Mollova, Nevena ^a   Leung, Kwan ^a   Chisholm, Jeffrey W ^a   Zablocki, Jeff ^a  

^a GILEAD SCIENCES   (United States)

^b Asinex Ltd   (Russian Federation)

^c N D ZELINSKY INSTITUTE OF ORGANIC CHEMISTRY   (Russian Federation)

^d ACCELRYS INC   (United States)

Author keywords

Delta 9 desaturase; Desaturase; HEPG2; Hydroxyacetamide; Liver triglycerides; Microsomal assay; Molecular overlay; SCD; Stearoyl CoA; Tissue partitioning; Tissue selectivity

Indexed keywords

ACYL COENZYME A DESATURASE; CVT 11563; CVT 12012; ENZYME INHIBITOR; MICROSOME ENZYME; OLEIC ACID; PALMITOLEIC ACID; SUCROSE; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; VACCENIC ACID;

ANIMAL EXPERIMENT; ARTICLE; BRAIN; CELL STRAIN HEPG2; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; GAS CHROMATOGRAPHY; HUMAN; HUMAN CELL; IN VIVO STUDY; LIPID COMPOSITION; LIVER; MALE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

ACETAMIDES; ADMINISTRATION, ORAL; ANIMALS; CELL LINE, TUMOR; CHEMISTRY, PHARMACEUTICAL; DOSE-RESPONSE RELATIONSHIP, DRUG; FATTY ACIDS; HUMANS; INHIBITORY CONCENTRATION 50; LIVER; MALE; MICROSOMES; RATS; RATS, SPRAGUE-DAWLEY; STEAROYL-COA DESATURASE; SUCROSE; TRIGLYCERIDES;

RATTUS;

EID: 67649909584     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.06.017     Document Type: Article

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