Synthesis and Evaluation of Quinazolin-4(3H)-one Derivatives as Multitarget Metabolic Enzyme Inhibitors: A Biochemistry-Oriented Drug Design
Yazarlar (4)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Doç. Dr. Parham Taslımı Bartın Üniversitesi, Türkiye
Morteza Sadeghi University of Isfahan, İran
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Chemistryselect (Q3) | ||
| Dergi ISSN | 2365-6549 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 07-2023 |
| Cilt / Sayı / Sayfa | 8 / 25 / – | DOI | 10.1002/slct.202301158 |
| Makale Linki | https://doi.org/10.1002/slct.202301158 | ||
| UAK Araştırma Alanları |
Organik Kimya
Spektroskopi
Biyokimya
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| Özet |
| In this study, imines bearing quinazolin‐4(3H)‐one were synthesized and their inhibitory properties were investigated against some metabolic enzymes including Acetylcholinesterase (AChE), Butyrylcholinesterase (BChE), α‐Glycosidase (α‐Gly), and human Carbonic Anhydrase I–II (hCA I–II). All compounds had inhibitory strength with Ki values in the range of 38.55±4.08–159.05±10.68 nM and 41.04±6.73–177.12±8.06 nM against hCA I and hCA‐II, respectively in comparison to the standard acetazolamide (AZA) Ki=125.15±0.78 nM (for hCA‐I) and Ki=148.75±0.92 nM (for hCA‐II). The compounds showed potent inhibitory activity against α‐Gly enzyme with IC50 value 0.34–2.28 nM (standard inhibitor acarbose (ACR): 3.18 nM). Also, these analogs had potent inhibitory strength with Ki values in the range of 4.20±0.15–26.10±2.36 nM against AChE and 1.22±0.05–16.09±0.88 nM against BChE in … |
| Anahtar Kelimeler |
| AChE | BChE | hCA I–II | molecular docking | quinazolin-4(3H)-one |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 56 |
| Scopus | 55 |
| Google Scholar | 64 |