1297595-95-9

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 
• 1238891-85-4 {3-bromo-2-[(2,3-dibromo-4,5-dimethoxyphenyl)methyl]-4,5-dimethoxyphenyl}methanol 
• 71-36-3 butan-1-ol 
• 1238891-84-3 2,3-dibromo-1-(2'-bromo-6'-bromomethyl-3',4'-dimethoxybenzyl)-4,5-dimethoxybenzene 

Relevant academic research and scientific papers

Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6- (isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice

In an effort to develop novel small molecule PTP1B inhibitors, a series of bromophenol derivatives were designed, synthesized and evaluated in vitro and in vivo. All of the synthesized compounds displayed weak to potent PTP1B inhibitory activities (5.62-96.25%) at 20 μg/mL. Among these compounds, 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol (9) exhibited enhanced PTP1B inhibitory activity (IC50 = 1.50 μM) than the lead compound BDDPM (IC50 = 2.42 μM) and high selectivity against other PTPs (TCPTP, LAR, SHP-1 and SHP-2). Results of anti-diabetic assay using C57BL/KsJ-db/db mouse model demonstrated that compound 9 was effective at lowering blood glucose, total cholesterol and HbA1c (P 0.01).

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.