Quinazolinone-based benzenesulfonamides with low toxicity and high affinity as monoamine oxidase-A inhibitors: Synthesis, biological evaluation and induced-fit docking studies
Yazarlar (9)
Doç. Dr. Cem Yamalı Çukurova Üniversitesi, Türkiye
Prof. Dr. Halise İnci Gül Atatürk Üniversitesi, Türkiye
Doç. Dr. Mehtap TUĞRAK SAKARYA Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Doç. Dr. Begüm Nurpelin Sağlık Türkiye
Prof. Dr. Abdulilah Ece Türkiye
Doç. Dr. Göksun Demirel Türkiye
Dr. Öğr. Üyesi Merve Nenni Türkiye
Dr. Öğr. Üyesi Serkan Levent Türkiye
Dr. Öğr. Üyesi Ahmet Cihat Öner Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic Chemistry (Q1) | ||
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Türkçe | Basım Tarihi | 01-2022 |
| Cilt / Sayı / Sayfa | 124 / 0 / 105822– | DOI | 10.1016/j.bioorg.2022.105822 |
| Makale Linki | http://dx.doi.org/10.1016/j.bioorg.2022.105822 | ||
| UAK Araştırma Alanları |
Farmasotik Kimya
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| 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 … |
| Anahtar Kelimeler |
BM Sürdürülebilir Kalkınma Amaçları
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| Google Scholar | 43 |