SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors

A potent and bioavailable SCD inhibitor, 3j was identified from optimization of a lead thiazole compound and its in vivo SCD inhibition studies are described. Elevated stearoyl-CoA desaturase (SCD) activity has been linked to a number of metabolic disorders including obesity and type II diabetes. Co...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-03, Vol.20 (5), p.1593-1597
Hauptverfasser:	Ramtohul, Yeeman K., Black, Cameron, Chan, Chi-Chung, Crane, Sheldon, Guay, Jocelyne, Guiral, Sébastien, Huang, Zheng, Oballa, Renata, Xu, Li-Jing, Zhang, Lei, Li, Chun Sing
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Biological and medical sciences Body weight gain prevention Desaturation index Dietary Fats Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - toxicity General and cellular metabolism. Vitamins Hep G2 Cells Humans Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - chemistry Hypoglycemic Agents - toxicity Insulin and glucose sensitivity Medical sciences Mice Mice, Inbred C57BL Oxadiazoles - chemical synthesis Oxadiazoles - chemistry Oxadiazoles - toxicity Pharmacology. Drug treatments SCD inhibitors Stearoyl-CoA Desaturase - antagonists & inhibitors Stearoyl-CoA Desaturase - metabolism Structure-Activity Relationship Thiazoles - chemical synthesis Thiazoles - chemistry Thiazoles - toxicity Weight Gain
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