Related Experiment Video
Updated: Jun 2, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding
Shinji Kamisuki1, Takashi Shirakawa, Akira Kugimiya
1Institute for Chemical Research, Kyoto University, Uji, Kyoto, Japan.
Abstract:
Fatostatin, a recently discovered small molecule that inhibits activation of sterol regulatory element-binding protein (SREBP), blocks biosynthesis and accumulation of fat in obese mice. We synthesized and evaluated a series of fatostatin derivatives. Our structure-activity relationships led to the identification of N-(4-(2-(2-propylpyridin-4-yl)thiazol-4-yl)phenyl)methanesulfonamide (24, FGH10019) as the most potent druglike molecule among the analogues tested. Compound 24 has high aqueous solubility and membrane permeability and may serve as a seed molecule for further development.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Inhibitors of Bacterial Protein Synthesis
Antihypertensive Drugs: Thiazide-Class Diuretics
Eukaryotic Transcription Inhibitors
Eukaryotic transcription inhibitors usually contain two distinct domains, a DNA...
Enzyme Inhibition
Inhibitors of Viral Protein Synthesis
