Format

Send to

Choose Destination
J Med Chem. 2011 Jul 14;54(13):4923-7. doi: 10.1021/jm200304y. Epub 2011 Jun 8.

Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.

Author information

1
Institute 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.

PMID:
21561152
PMCID:
PMC3136361
DOI:
10.1021/jm200304y
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for American Chemical Society Icon for PubMed Central
Loading ...
Support Center