Novel Isoindole‐1,3‐Dione‐Isoxazole Hybrids: Synthesis, Characterization, Evaluation of Their Inhibitory Activities on Carbonic Anhydrase and Acetylcholinesterase
      
Yazarlar (5)
Özlem Gündoğdu Aytaç Kırşehir Ahi Evran Üniversitesi, Türkiye
Hilal Başak Gündoğdu
Atatürk Üniversitesi, Türkiye
Sertan Aytaç Kırşehir Ahi Evran Üniversitesi, Türkiye
Dr. Öğr. Üyesi Zeynebe BİNGÖL Tokat Gaziosmanpaşa Üniversitesi, Türkiye
İlhami Gülçin Atatürk Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı Journal of Biochemical and Molecular Toxicology (Q2)
Dergi ISSN 1095-6670 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili Türkçe Basım Tarihi 10-2025
Cilt / Sayı / Sayfa 39 / 10 / – DOI 10.1002/jbt.70550
Makale Linki https://doi.org/10.1002/jbt.70550
Özet
It is known that compounds containing isoxazole units exhibit a high potential for biological activity due to the isoxazole ring. In this study, eight hexahydro‐5H‐isoxazolo[4,5‐f]isoindole‐5,7(6H)‐dione derivatives bearing isoxazole moieties were synthesized and their inhibitory effects on various metabolic enzymes, including acetylcholinesterase (AChE) and human carbonic anhydrase isoforms I and II (hCA I and hCA II), which are associated with global disorders such as Alzheimer's disease (AD), epilepsy, and glaucoma, were investigated. Among the synthesized compounds, derivatives 9–12 exhibited notable inhibitory activity against AChE, hCA I, and hCA II enzymes. The IC50 values were determined to be in the ranges of 4.65–12.83 nM for AChE, 23.17–79.58 nM for hCA I, and 36.58–88.28 nM for hCA II. Molecular docking studies of the synthesized compounds 9a–12a were carried out against three …
Anahtar Kelimeler
acetylcholinesterase | carbonic anhydrase | inhibition effects | isoindole-1,3-dione | isoxazole ring