[Synthesis of (2'-bromo-4', 5'-dimethoxy-phenyl)-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane as PTP1B inhibitor].
OBJECTIVE
To synthesize (2'-bromo-4',5'-dimethoxy-phenyl)-( 2,3- dibromo-4,5-dimethoxy-phenyl)-methane (6) as protein tyrosine phosphatase 1B (PTP1B) inhibitor.


METHODS
Compound 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.


RESULTS
Compound 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.


CONCLUSIONS
The 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)).
Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China.
Jing
J
Li
Shuju
S
Guo
Hua
H
Su
Dayong
D
Shi
Lijun
L
Han
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D007700:Kinetics; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1