SYNTHESIS, CHARACTERIZATION AND CHOLINESTERASE INHIBITORY EFFECTS OF IBUPROFEN-BASED SPIROTHIAZOLIDINONES

Authors : Çağla Begüm Apaydın, Gozde Hasbal Çelikok, Tuğba Yılmaz Özden

Pages : 12-20

Doi:10.33483/jfpau.1493082

View : 61 | Download : 105

Publication Date : 2025-01-20

Article Type : Research Paper

Abstract :Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors for Alzheimer\\\'s disease therapy. Material and Method: In this study, novel spirocyclic compounds were synthesized by one-pot reaction. IR, 1H NMR, 13C NMR, LC-MS and elemental analysis techniques have all been used to clarify the chemical structures of the compounds. AChE and BuChE inhibitory effects of compounds (4a-e and, 5a-e) were assayed according to Ellman’s method using galantamine as reference. Result and Discussion: According to the inhibition data, compound 4e demonstrated the most promising activity against AChE, with an IC50 value of 39.53±1.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.97±1.79 µM.
Keywords : Asetilkolinesteraz, butirilkolinesteraz, ibuprofen, sentez, spirotiyazolidinon