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


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Ertik O., KOLANCILAR H., YANARDAĞ R.

Indian Journal of Chemistry (IJC), vol.63, no.3, pp.253-262, 2024 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 63 Issue: 3
  • Publication Date: 2024
  • Doi Number: 10.56042/ijc.v63i3.5887
  • Journal Name: Indian Journal of Chemistry (IJC)
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.253-262
  • Keywords: ADME, Benzochromone, Benzocoumarin, Enzyme inhibition, Molecular docking
  • Open Archive Collection: AVESIS Open Access Collection
  • Istanbul University Affiliated: Yes

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.