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    Novel Quinazolinone Derivatives: Potential Synthetic Analogs for the Treatment of Glaucoma, Alzheimer's Disease and Diabetes Mellitus
    (Wiley-V C H Verlag Gmbh, 2023) Tokali, Feyzi Sinan; Taslimi, Parham; Tuzun, Burak; Karakus, Ahmet; Sadeghian, Nastaran; Gulcin, Ilhami
    Quinazolinones, which represent an important part of nitrogen-containing six-membered heterocyclic compounds, are frequently used in drug design due to their wide biological activity properties. Therefore, the novel quinazolinones were synthesized from the reaction of acylated derivatives of 4-hydroxy benzaldehyde with 3-amino-2-alkylquinazolin-4(3H)-ones with good yields (85-94 %) and their structures were characterized using Fourier-transform Infrared (FT-IR), Nuclear Magnetic Resonance ((1) H-NMR, (13) C-NMR), and High-Resolution Mass Spectroscopy (HR-MS). As the application of the synthesized compounds, their inhibition properties of the synthesized compounds on alpha-Glucosidase (alpha-Glu), Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), and Carbonic anhydrase I-II (hCA I-II) metabolic enzymes were investigated. All compounds showed inhibition at nanomolar level with the K-i values in the range of 12.73 +/- 1.26-93.42 +/- 9.44 nM for AChE, 8.48 +/- 0.92-25.84 +/- 2.59 nM for BChE, 66.17 +/- 5.16-818.06 +/- 44.41 for alpha-Glu, 2.56 +/- 0.26-88.23 +/- 9.72 nM for hCA I, and 1.68 +/- 0.14-85.43 +/- 7.41 nM for hCA II. Molecular docking study was performed to understand the interactions of the most potent compounds with corresponding enzymes. Also, absorption, distribution, metabolism, excretion, and toxicity (ADME/T) properties of the compounds were investigated.
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    Synthesis of new carboxylates and sulfonates containing thiazolidin-4-one ring and evaluation of inhibitory properties against some metabolic enzymes
    (Springer, 2023) Tokali, Feyzi Sinan; Taslimi, Parham; Tuzun, Burak; Karakus, Ahmet; Sadeghian, Nastaran; Gulcin, Ilhami
    A series of thizaolidin-4-one derivatives (3a-o) was synthesized with excellent yield (94-97%) and the structures of the compounds were characterized with Fourier-transform Infrared (FTIR), Nuclear Magnetic Resonance (H-1 NMR-C-13 NMR), and High-resolution Mass Spectroscopy (HRMS). Novel compounds were tested towards some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I-II (hCA I-II). All the synthetic analogs had potent inhibitory strength with Ki values in the range of 161.28 +/- 16.91-943.13 +/- 57.23nM against hCA-I and 151.77 +/- 21.42-879.89 +/- 57.70 nM against hCA-II in comparison to the standard acetazolamide K-i = 847.18 +/- 75.41nM (for hCA-I) and Ki = 776.12 +/- 70.62nM (for hCA-II). Most of the compounds showed potent inhibitory activity against AChE and BChE enzymes with IC50 value 823.71-984.32 nM, 321.88-879.02 nM, 2.61-83.08 nM compared to the standard compounds (928.85, 691.41, and 68.85 nM), respectively. Additionally, the molecular docking study was carried out for the most active compound for the determination of ligand-enzyme interactions. Also, the Absorption, Distribution, Metabolism, Excretion and Toxicity (ADME/T) properties of the molecules were calculated. [GRAPHICS] .