1297595-98-2

Upstream product

• 70625-29-5 2,3-dibromo-4,5-dimethoxybenzaldehyde 
• 1273542-60-1 2,3-dibromo-1-(2'-bromo-3',4'-dimethoxy-6'-methylbenzyl)-4,5-dimethoxy benzene 
• 2973-76-4 5-bromo-4-hydroxy-3-methoxybenzaldehyde 
• 121-33-5 vanillin 
• 6948-30-7 5-bromoveratralaldehyde 
• 68278-85-3 3-bromo-4,5-dimethoxy-toluene 
• 4950-08-7 (2,3-dibromo-4,5-dimethoxyphenyl)methanol 
• 91-16-7 1,2-dimethoxybenzene 
• 1238891-85-4 {3-bromo-2-[(2,3-dibromo-4,5-dimethoxyphenyl)methyl]-4,5-dimethoxyphenyl}methanol 
• 1238891-84-3 2,3-dibromo-1-(2'-bromo-6'-bromomethyl-3',4'-dimethoxybenzyl)-4,5-dimethoxybenzene 

Downstream Products

• 1297595-97-1 2,3-dibromo-1-[2'-bromo-6'-(2-bromo-4,5-dimethoxybenzyl)-3',4'-dimethoxybenzyl]-4,5-dimethoxybenzene 
• 1378399-14-4 3,4-dibromo-5-(2-bromo-6-(3,4-dihydroxybenzyl)-3,4-dihydroxybenzyl)benzene-1,2-diol 

Relevant academic research and scientific papers

PTP1B INHIBITORS, SYNTHESIS THEREOF AND APPLICATION THEREOF IN PREPARATION OF MEDICAMENTS FOR TREATING TYPE 2 DIABETES MELLITUS

The present invention relates to chemical total synthesis methods of six novel protein tyrosine phosphatase-1B (PTP1B) inhibitors and application of the inhibitors in the preparation of medicaments for treating type 2 diabetes mellitus (T2DM). The PTP1B inhibitors use one or more of the six compounds represented by the structural formulae 1, 2, 3, 4, 5 and 6, as active components. The compounds can enhance the sensitivity of an insulin receptor by inhibiting the activity of PTP1B, thereby having a favorable therapeutic effect on insulin-resistant T2DM.

Design, synthesis, and biological evaluation of bromophenol derivatives as protein tyrosine phosphatase 1B inhibitors

3-Bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a bromophenol purified from the marine red alga Rhodomela confervoides and exhibits potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC 50 = 1.7 μmol/L). In an effort to improve the PTP1B inhibitory activity, a series of derivatives were designed, synthesized, and evaluated in vitro. The preliminary structure-activity relationship indicated that the tricyclic scaffold and multi-bromine atoms (four to five) attached to the aryl rings are important for PTP1B inhibition. Among these, compound 26 exhibited remarkable inhibitory activity against PTP1B with an IC50 of 0.89 μmol/L, which was approximately two-fold more potent than the initial lead compound BDB.