Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity

SCD1 is a rate-limiting enzyme in the conversion of saturated fatty acids to monounsaturated fatty acids. SCD1 inhibitors have potential effects on obesity, diabetes, acne, and cancer, but the adverse effects associated with SCD1 inhibition in the skin and eyelids are impediments to clinical develop...

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Veröffentlicht in:	European journal of medicinal chemistry 2018-10, Vol.158, p.832-852
Hauptverfasser:	Iida, Tetsuya, Ubukata, Minoru, Mitani, Ikuo, Nakagawa, Yuichi, Maeda, Katsuya, Imai, Hiroto, Ogoshi, Yosuke, Hotta, Takahiro, Sakata, Shohei, Sano, Ryuhei, Morinaga, Hisayo, Negoro, Tamotsu, Oshida, Shinichi, Tanaka, Masahiro, Inaba, Takashi
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetic Acid - chemistry Acetic Acid - pharmacology Animals Diabetes Mellitus - drug therapy Diabetes Mellitus - enzymology Diabetes Mellitus - metabolism Drug Discovery Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Liver - drug therapy Fatty Liver - enzymology Fatty Liver - metabolism Liver - drug effects Liver - enzymology Liver - metabolism Liver-selective SCD1 inhibitor Male Mice, Inbred C57BL Obesity - drug therapy Obesity - enzymology Obesity - metabolism Physicochemical properties Rats Rats, Sprague-Dawley Stearoyl-CoA Desaturase - antagonists & inhibitors Stearoyl-CoA Desaturase - metabolism Stearoyl-CoA desaturase 1 Thiazole-4-acetic acid derivative Thiazoles - chemistry Thiazoles - pharmacology
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