| Yazarlar |
Doç. Dr. Feyzi Sinan TOKALI
Türkiye |
Yeliz Demir
Türkiye |
|
İbrahim Hakkı Demircioğlu
Türkiye |
|
Cüneyt Türkeş
Türkiye |
Doç. Dr. Erbay KALAY
Kafkas Üniversitesi, Türkiye |
Prof. Dr. Kıvılcım ŞENDİL
Türkiye |
|
Şükrü Beydemir
Türkiye |
| Özet |
| A series of novel sulfonates containing quinazolin-4(3H)-one ring derivatives was designed to inhibit aldose reductase (ALR2, EC 1.1.1.21). Novel quinazolinone derivatives (1-21) were synthesized from the reaction of sulfonated aldehydes with 3-amino-2-alkylquinazolin-4(3H)-ones in glacial acetic acid with good yields (85%-94%). The structures of the novel molecules were characterized using IR, H-NMR, C-NMR, and HRMS. All the novel quinazolinones (1-21) demonstrated nanomolar levels of inhibitory activity against ALR2 (K s are in the range of 101.50-2066.00 nM). Besides, 4-[(2-isopropyl-4-oxoquinazolin-3[4H]-ylimino)methyl]phenyl benzenesulfonate (15) showed higher inhibitor activity inhibited ALR2 up to 7.7-fold compared to epalrestat, a standard inhibitor. Binding interactions between ALR2 and quinazolinones have been investigated using Schrödinger Small-Molecule Drug Discovery Suite 2021-1, reported possible inhibitor-ALR2 interactions. Both in vitro and in silico study results suggest that these quinazolin-4(3H)-one ring derivatives (1-21) require further molecular modification to improve their drug nominee potency as an ALR2 inhibitor. |
| Anahtar Kelimeler |
| ADME-Tox,aldose reductase,epalrestat,in silico study,molecular docking,quinazolinones |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | DRUG DEVELOPMENT RESEARCH |
| Dergi ISSN | 0272-4391 |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q2 |
| Makale Dili | İngilizce |
| Basım Tarihi | 01-2022 |
| Cilt No | 83 |
| Sayı | 3 |
| Sayfalar | 586 / 604 |
| Doi Numarası | 10.1002/ddr.21887 |
| Makale Linki | https://onlinelibrary.wiley.com/doi/epdf/10.1002/ddr.21887 |
| Atıf Sayıları | |
| WoS | 65 |
