Biological and computational evaluation of novel benzofuranyl derivatives asacetylcholinesterase and butyrylcholinesterase inhibitors
 
Yazarlar (5)
Makale Türü Açık Erişim Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı FUTURE MEDICINAL CHEMISTRY (Q2)
Dergi ISSN 1756-8919 Dergi Bilgileri (2024)
Dergi Tarandığı Indeksler SSCI
Makale Dili İngilizce Basım Tarihi 06-2024
Kabul Tarihi Yayınlanma Tarihi 30-05-2024
Cilt / Sayı / Sayfa 16 / 11 / 1075–1085 DOI 10.1080/17568919.2024.2342641
Makale Linki https://www.tandfonline.com/doi/epdf/10.1080/17568919.2024.2342641?needAccess=true
UAK Araştırma Alanları
Biyokimya Organik Kimya Spektroskopi
Özet
Aim A highly efficient one-step method has been developed for the synthesis of benzofuranyl derivatives from 2-benzoylcyclohexane-1-carboxylic acid derivatives using chlorosulfonyl isocyanate. This novel method provides a practical, cost-effective and efficient approach. Materials & methods The inhibitory effects of benzofuranyl derivatives on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes were investigated. Ki values were determined to range from 0.009 to 0.61 μM for AChE and 0.28 to 1.60 μM for BChE. Molecular docking analysis provided insights into the interaction modes and binding patterns of these compounds with AChE and BChE. Conclusion Kinetic findings of our study suggest that some of our compounds exhibited more effective low micromolar inhibition compared with the reference, and these derivatives could be used to design more powerful agents.
Anahtar Kelimeler
acetylcholinesterase | Alzheimer's disease | benzofuranyl | butyrylcholinesterase | molecular modeling