| Yazarlar (6) |
Doç. Dr. Feyzi Sinan TOKALI
Kafkas Üniversitesi, Türkiye |
Parham Taslımı
Bartın Üniversitesi, Türkiye |
|
Burak Tüzün
Sivas Cumhuriyet Üniversitesi, Türkiye |
|
Ahmet Karakuş
Bartın Üniversitesi, Türkiye |
|
Nastaran Sadeghıan
Bartın Üniversitesi, Türkiye |
|
İlhami Gülçin
Atatürk Üniversitesi, Türkiye |
| Özet |
| 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 ( H-NMR, C-NMR), and High-Resolution Mass Spectroscopy (HR-MS). As the application of the synthesized compounds, their inhibition properties of the synthesized compounds on α-Glucosidase (α-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 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 α-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. |
| Anahtar Kelimeler |
| cholinesterases | diabetes | quinazolin-4(3H)-one | molecular docking | ADME/T |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | Chemistry & Biodiversity |
| Dergi ISSN | 1612-1872 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q3 |
| Makale Dili | İngilizce |
| Basım Tarihi | 10-2023 |
| Cilt No | 20 |
| Sayı | 10 |
| Doi Numarası | 10.1002/cbdv.202301134 |
| Makale Linki | http://dx.doi.org/10.1002/cbdv.202301134 |
| Atıf Sayıları | |
| WoS | 23 |
