Discovery of thiazolylpyridinone SCD1 inhibitors with preferential liver distribution and reduced mechanism-based adverse effects

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 2, 2014, Pages 526-531

  Sun, Shaoyi ^a   Zhang, Zaihui ^a   Raina, Vandna ^a   Pokrovskaia, Natalia ^a   Hou, Duanjie ^a   Namdari, Rostam ^a   Khakh, Kuldip ^a   Ratkay, Leslie G ^a   McLaren, David G ^a   Mork, Monica ^a   Fu, Jianmin ^a   Ferreira, Suzie ^b   Hubbard, Brian ^b   Winther, Michael D ^a   Dales, Natalie ^b  

^a Xenon Pharmaceuticals Inc   (Canada)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Desaturation index; Liver selective; SCD1 inhibitors; Stearoyl CoA desaturase 1; Thiazolylpyridinone

Indexed keywords

2 AMINOTHIAZOLE; ACYL COENZYME A DESATURASE 1; BENZYL DERIVATIVE; OXYGENASE INHIBITOR; PYRIDONE DERIVATIVE; THIAZOLYLPYRIDINONE; UNCLASSIFIED DRUG; ACYL COENZYME A DESATURASE; STEAROYL COA DESATURASE 1;

ABSENCE OF SIDE EFFECTS; ADVERSE DRUG REACTION; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CELL ASSAY; CELL MEMBRANE PERMEABILITY; CLINICAL OBSERVATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG DOSE; DRUG LIVER LEVEL; DRUG MECHANISM; DRY EYE; DRY SKIN; FEMALE; HYPOTHESIS; IC 50; IN VITRO STUDY; IN VIVO STUDY; LEWIS RAT; LIVER MICROSOME; MOUSE; NONHUMAN; RAT; RISK ASSESSMENT; STRUCTURE ACTIVITY RELATION; CACO 2 CELL LINE; DRUG DISTRIBUTION; DRUG SAFETY; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROLYSIS; TISSUE DISTRIBUTION;

DESATURATION INDEX; LIVER SELECTIVE; SCD1 INHIBITORS; STEAROYL-COA DESATURASE-1; THIAZOLYLPYRIDINONE;

ANIMALS; CACO-2 CELLS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HEP G2 CELLS; HUMANS; LIVER; MICE; PYRIDONES; RATS; RATS, INBRED LEW; STEAROYL-COA DESATURASE; TISSUE DISTRIBUTION;

EID: 84891861970     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.12.035     Document Type: Article

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