Síntese, caracterização e avaliação biológica de compostos heterocíclicos

Abstract

The present work describes the synthesis, characterization and in vitro biological evaluation of molecular hybrid compounds. The first part involved molecular docking, where molecular hybrids, derivatives of 4-aminoquinoline and sulfonamides were highlighted in a screening carried out with more than 150 compounds synthesized by the research group against the inhibition of the replication of the SARS-CoV-2 virus and in the inhibition of the acetylcholinesterase, βsecretase and glycogen synthase kinase 3β enzymes, related to Alzheimer's disease (AD). The assays involving the inhibition of replication of the SARS-CoV-2 virus showed promising results, as the inhibition exceeded 95% for some of the compounds, at a concentration of 10 µM. Regarding the biological tests involving ADrelated enzymes, compound 8 showed high inhibition in the three enzymes and became a promising multi-target enzymatic inhibitor in the treatment of this disease. The second part involves molecular hybrid compounds derived from alkylated 1,2,3- triazoles with acridine or purine, as well as their in vitro antileishmanial evaluation.