1297595-94-8

Upstream product

• 6948-30-7 5-bromoveratralaldehyde 
• 121-33-5 vanillin 
• 2973-76-4 5-bromo-4-hydroxy-3-methoxybenzaldehyde 
• 1273542-60-1 2,3-dibromo-1-(2'-bromo-3',4'-dimethoxy-6'-methylbenzyl)-4,5-dimethoxy benzene 
• 70625-29-5 2,3-dibromo-4,5-dimethoxybenzaldehyde 
• 4950-08-7 (2,3-dibromo-4,5-dimethoxyphenyl)methanol 
• 68278-85-3 3-bromo-4,5-dimethoxy-toluene 
• 1238891-85-4 {3-bromo-2-[(2,3-dibromo-4,5-dimethoxyphenyl)methyl]-4,5-dimethoxyphenyl}methanol 
• 67-63-0 isopropyl alcohol 

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.

HPN, a synthetic analogue of bromophenol from red alga Rhodomela confervoides: Synthesis and anti-diabetic effects in C57BL/KsJ-db/db mice

3,4-Dibromo-5-(2-bromo-3,4-dihydroxy-6-(isopropoxymethyl)benzyl)benzene-1, 2-diol (HPN) is a synthetic analogue of 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6- (ethoxymethyl)benzyl)benzene-1,2-diol (BPN), which is isolated from marine red alga Rhodomela confervoides with potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC50 = 0.84 μmol/L). The in vitro assay showed that HPN exhibited enhanced inhibitory activity against PTP1B with IC50 0.63 μmol/L and high selectivity against other PTPs (T cell protein tyrosine phosphatase (TCPTP), leucocyte antigen-related tyrosine phosphatase (LAR), Src homology 2-containing protein tyrosine phosphatase-1 (SHP-1) and SHP-2). The results of antihyperglycemic activity using db/db mouse model demonstrated that HPN significantly decreased plasma glucose (P a dose-dependent manner. Besides, both of the high and medium dose groups of HPN remarkably decreased HbA1c levels (P a similar antihyperglycemic activity as rosiglitazone. HPN therefore have potential for development as treatments for Type 2 diabetes.