| Yazarlar (8) |
Dr. Öğr. Üyesi Songül BOY
Kafkas Üniversitesi, Türkiye |
Abdülmelik Aras
Iğdır Üniversitesi, Türkiye |
|
Fikret Türkan
Iğdır Üniversitesi, Türkiye |
Doç. Dr. Onur AKYILDIRIM
Kafkas Üniversitesi, Türkiye |
Doç. Dr. Murat BEYTUR
Kafkas Üniversitesi, Türkiye |
|
Halide Sedef Karaman
Türkiye |
Doç. Dr. Sevda MANAP
Kafkas Üniversitesi, Türkiye |
Prof. Dr. Haydar YÜKSEK
Kafkas Üniversitesi, Türkiye |
| Özet |
| In the present study, 3-substitued-4-(4-hydroxybenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (S1-8) were synthesized by treating 4-hydroxybenzaldehyde (B) with eight different 3-substitued-4-amino-4,5-dihydro-1H-1,2,4-triazole-5-ones (T1-8) in acetic acid medium, separately. The synthesized Schiff bases (S) were reacted with formaldehyde and secondary amine such as 4-piperidinecarboxyamide to afford novel heterocyclic bases. 3-Substitued-4-(4-hydroxybenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (T) were treated with 4-piperidinecarboxyamide in the presence of formaldehyde to synthesize eight new 1-(4-piperidinecarboxyamide-1-yl-methyl)-3-substitued-4-(4-hydroxybenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (M1-8). The structure characterization of compounds was carried out using 1H-NMR, IR, HR-MS, and 13C-NMR spectroscopic methods. The inhibitory properties of the newly synthesized compounds were calculated against the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and glutathione S-transferase (GST) enzymes. Ki values were calculated in the range of 20.06±3.11–36.86±6.17 μM for GST, 17.87±2.91–30.53±4.25 μM for AChE, 9.08±0.69–20.02±2.88 μM for BChE, respectively, Besides, IC50 values were also calculated. Best binding scores of -inhibitors against used enzymes were calculated as −12.095 kcal/mol, −12.775 kcal/mol, and −9.336 kcal/mol, respectively. While 5-oxo-triazole piperidine-4-carboxamide moieties have a critical role in the inhibition of AChE and GST enzymes, hydroxy benzyl moiety is important for BChE enzyme inhibition. |
| Anahtar Kelimeler |
| 4-piperidinecarboxyamide | docking study | heterocyclic bases | inhibitory activity | schiff base |
| 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 | Türkçe |
| Basım Tarihi | 10-2021 |
| Cilt No | 18 |
| Sayı | 11 |
| Doi Numarası | 10.1002/cbdv.202100433 |
| Makale Linki | http://dx.doi.org/10.1002/cbdv.202100433 |
| Atıf Sayıları | |
| SCOPUS | 19 |
| Google Scholar | 25 |
