Quinazolinone-based benzenesulfonamides with low toxicity and high affinity as monoamine oxidase-A inhibitors: Synthesis, biological evaluation and induced-fit docking studies
Yazarlar (9)
Çukurova Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Doç. Dr. Mehtap TUĞRAK SAKARYA
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Türkiye
Türkiye
Türkiye
Türkiye
Türkiye
Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Bioorganic Chemistry |
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q1 |
| Makale Dili | Türkçe |
| Basım Tarihi | 01-2022 |
| Cilt No | 124 |
| Sayfalar | 105822 / |
| DOI Numarası | 10.1016/j.bioorg.2022.105822 |
| Makale Linki | http://dx.doi.org/10.1016/j.bioorg.2022.105822 |
| Özet |
| The research in selective monoamine oxidases (MAO-A and MAO-B) inhibitors has been increased due to their therapeutic value for neurodegenerative diseases. In this study, 4-((2-(aryl)-4-oxoquinazolin-3(4H)-yl)amino)benzenesulfonamides were synthesized and their MAOs inhibition potentials were investigated applying in vitro fluorometric technique. The most potent compounds 7 and 8 against MAO-A had IC50 values of 0.058 ± 0.002 and 0.094 ± 0.003 µM, respectively, while the reference moclobemide had an IC50 value of 6.061 µM. Compounds 7 (>1724 times) and 8 (>1063 times) more selective and reversible inhibitors of MAO-A rather than MAO-B. Toxicity studies of 7 (IC50 = 210.23 µM) and 8 (IC50 = 259.27 µM) showed that compounds can be considered as non-toxic towards SH-SY5Y cell line at their effective concentrations against MAO-A. In silico docking simulations successfully explained the … |
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BM Sürdürülebilir Kalkınma Amaçları
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| Google Scholar | 40 |