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

We discovered a series of novel and potent thiazolylpyridinone-based SCD1 inhibitors based on a 2-aminothiazole HTS hit by replacing the amide bond with a pyridinone moiety. Compound 19 demonstrated good potency against SCD1 in vitro and in vivo. The mouse liver microsomal SCD1 in vitro potency for...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-01, Vol.24 (2), p.526-531
Hauptverfasser:	Sun, Shaoyi, Zhang, Zaihui, Raina, Vandna, Pokrovskaia, Natalia, Hou, Duanjie, Namdari, Rostam, Khakh, Kuldip, Ratkay, Leslie G., McLaren, David G., Mork, Monica, Fu, Jianmin, Ferreira, Suzie, Hubbard, Brian, Winther, Michael D., Dales, Natalie
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Caco-2 Cells Desaturation index Dose-Response Relationship, Drug Drug Discovery - methods Eyelid Hep G2 Cells Humans Liver - drug effects Liver - metabolism Liver selective Mice Pyridones - chemistry Pyridones - metabolism Pyridones - pharmacology Rats Rats, Inbred Lew SCD1 inhibitors Stearoyl-CoA Desaturase - antagonists & inhibitors Stearoyl-CoA Desaturase - metabolism Stearoyl-CoA desaturase-1 Thiazolylpyridinone Tissue Distribution - drug effects Tissue Distribution - physiology
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