Synthesis of some benzocoumarin and benzochromone: Antielastase, antihyaluronidase, anticollagenase and antidiabetic activities and in silico ADME and molecular docking studies

Abstract

Coumarins are compounds commonly found in nature and have many biological effects. So it is a molecule that continues to be popular. Benzocoumarin and benzochromone, which are coumarin derivatives, are a group of molecules obtained from plants and it is important to understand the biological activity of the derivatives of these molecules. In our study, the inhibitory effects of newly synthesized 9-hydroxy-1-methyl-3H-naphto[2,1-b]piran-3-on (benzocoumarin) (1) and 9-hydroxy-2-methyl-4H-naphto[2,1-b]piran-4-on (benzochromone) (2) on elastase, hyaluronidase, collagenase, alpha-amylase, and alpha-glucosidase were investigated. As a result of in vitro studies, the inhibition effect of compounds 1 (132.64±16.12 µM) and 2 (400.25±64.77 µM)), was observed relative to the dose, only the inhibition effect on collagenase was found to have a lower IC₅₀ value than the positive control (479.03±38.40 µM). In line with the data obtained as a result of in vitro studies, molecular docking studies were also carried out for compounds 1 and 2 with collagenase. As a result, due to the inhibitory effect of compounds 1 and 2 on the collagenase activity, a way has been opened for further studies to prove it.