Systematic evaluation of amide bioisosteres leading to the discovery of novel and potent thiazolylimidazolidinone inhibitors of SCD1 for the treatment of metabolic diseases

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 2, 2014, Pages 520-525

  Sun, Shaoyi ^a   Zhang, Zaihui ^a   Kodumuru, Vishnumurthy ^a   Pokrovskaia, Natalia ^a   Fonarev, Julia ^a   Jia, Qi ^a   Leung, Po Yee ^b   Tran, Jennifer ^b   Ratkay, Leslie G ^a   McLaren, David G ^a   Radomski, Chris ^a   Chowdhury, Sultan ^a   Fu, Jianmin ^a   Hubbard, Brian ^b   Winther, Michael D ^a   Dales, Natalie A ^b  

^a Xenon Pharmaceuticals Inc   (Canada)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Amide bioisosteres; Desaturation index; SCD1 inhibitors; Stearoyl CoA desaturase 1; Thiazolylimidazolidinone

Indexed keywords

2 AMINOTHIAZOLE; ACYL COENZYME A DESATURASE 1; AMIDE; AMYL NITRITE; BENZYL BROMIDE; HYDROXYLAMINE; ISOXAZOLE; OXYGENASE INHIBITOR; UNCLASSIFIED DRUG; XEN 723; 2 AMINOTHIAZOLE DERIVATIVE; ACYL COENZYME A DESATURASE; ACYL COENZYME A DESATURASE INHIBITOR;

ALKYLATION; ANIMAL CELL; ARTICLE; CATALYSIS; CROSS COUPLING REACTION; CYCLIZATION; DRUG SYNTHESIS; HYDROLYSIS; IN VITRO STUDY; METABOLIC DISORDER; NONHUMAN; SUZUKI REACTION; ANIMAL EXPERIMENT; CONCENTRATION RESPONSE; DRUG POTENCY; DRUG SCREENING; DRUG TOLERABILITY; EC50; FATTY ACID DESATURATION; FEMALE; HEPG2 CELL LINE; HUMAN; HUMAN CELL; IC50; LIVER MICROSOME; RAT;

AMIDE BIOISOSTERES; DESATURATION INDEX; SCD1 INHIBITORS; STEAROYL-COA DESATURASE-1; THIAZOLYLIMIDAZOLIDINONE;

AMIDES; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; FEMALE; HEP G2 CELLS; HUMANS; IMIDAZOLIDINES; METABOLIC DISEASES; MICE; RATS; RATS, SPRAGUE-DAWLEY; STEAROYL-COA DESATURASE;

EID: 84891876617     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.12.036     Document Type: Article

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