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), cilt.63, sa.3, ss.253-262, 2024 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 63 Sayı: 3
  • Basım Tarihi: 2024
  • Doi Numarası: 10.56042/ijc.v63i3.5887
  • Dergi Adı: Indian Journal of Chemistry (IJC)
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.253-262
  • Anahtar Kelimeler: ADME, Benzochromone, Benzocoumarin, Enzyme inhibition, Molecular docking
  • Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
  • İstanbul Üniversitesi Adresli: Evet

Özet

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.