Metabolic syndrome (MS) is a complex disease in which diabetes, obesity, hyperglycemia, high cholesterol and high blood pressure are the most common disorders. It is estimated that around 20-25 % of the world’s adult population have metabolic syndrome and they are twice as likely to die from some of their complications and three times as likely to have a heart attack or stroke compared with people without the syndrome. Currently, the research of multi-target drugs has been a challenging task in medicinal chemistry, and it has been proposed as an interesting approach to develop drugs aimed to treat complex diseases. In our group, we have evaluated some anthranilic acid derivatives in silico as potential ligands to some biological targets related to MS. Compound MABJ 1-48 was identified as a potential multi-target drug, as it showed high docking scores against aldose reductase, PDE5, PPAR-α, PPAR-γ and HMG-CoA. Its in silico pharmacokinetic profile was calculated, suggesting this molecule may have good ADME-Tox profile, including high oral absorption. This compound was synthesized and fully characterized by IR, 1H NMR, 13C NMR and MS. Finally, it was biological evaluated in a diet-induced obesity rat model and significantly lowered glucose levels. Hence, MABJ 1-48 is an interesting starting point for the development of new multitarget drugs for MS.

Anthranilic acid derivatives as potential multi-target drugs for metabolic syndrome treatment

253rd National Meeting (2017)

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