Synthesis of (2'-bromo-4', 5'-dimethoxy-phenyl)-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane as PTP1B inhibitor.
- Author:
Jing LI
1
;
Shuju GUO
;
Hua SU
;
Dayong SHI
;
Lijun HAN
Author Information
- Publication Type:Journal Article
- MeSH: Enzyme Inhibitors; chemical synthesis; chemistry; Kinetics; Protein Tyrosine Phosphatase, Non-Receptor Type 1; antagonists & inhibitors
- From: China Journal of Chinese Materia Medica 2009;34(12):1516-1519
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo synthesize (2'-bromo-4',5'-dimethoxy-phenyl)-( 2,3- dibromo-4,5-dimethoxy-phenyl)-methane (6) as protein tyrosine phosphatase 1B (PTP1B) inhibitor.
METHODCompound 6 was synthesized by Friedel-Crafts reaction, bromination and decarbonylation and screened inhibitory activity against PTP1B by the colorimetric assay. The structure of synthetic intermediates and target product were identified on the basis of spectral analysis.
RESULTCompound 6 was synthesized successfully in four steps and evaluated for its PTP1B inhibitory activity, the screening result shown that compound 6 displayed good inhibitory activity against PTP1B.
CONCLUSIONThe target compound 6 was synthesized with the overall yield of 20%, which was a new compound and shown good inhibitory activity against PTP1B (inhibition 40.16% at 5 mg x L(-1)).
