Metabolic syndrome (MetS) 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 adult population worldwide has MetS and they are twice as likely to die from some of their complications compared to people without the syndrome. Currently, the research of multitarget drugs has been a challenging task in medicinal chemistry, and it has been proposed as an interesting approach for developing drugs for the treatment of complex diseases. In our group, we have studied anthranilic acid derivatives as potential drugs for the management of some metabolic disorders. In this work, we present the in silico and the in vivo evaluation of HGA-01. This compound was identified as a potential multitarget drug from an inverse docking study carried out on several targets involved in MetS, showing high theoretical affinity to aldose reductase, PPAR-α, PPAR-γ, and HMG-CoA reductase. HGA-01 was prepared from anthranilic acid in just four steps with good yields. Then, it was evaluated in a diet-induced obesity rat model and induced diminution in blood pressure, glucose, triglycerides, and cholesterol levels compared with the untreated group. Hence, HGA-01 is an interesting advance for the development of new multitarget drugs for the management of MetS.

Design, synthesis, and evaluation of the anthranilic acid derivative HGA-01 as a potential multitarget drug for the management of metabolic syndrome

2019 Spring National Meeting

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