Targeting cholinergic dysfunction and neuroinflammation through rationally designed Thieno[3,2-d]pyrimidine hybrids
Yazarlar (7)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Öğr. Gör. Özden Özgün Acar Pamukkale Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Arş. Gör. Büşra Acar Abdullah Gül Üniversitesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Prof. Dr. Alaattin Şen Pamukkale Üniversitesi, 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 | İngilizce | Basım Tarihi | 07-2026 |
| Cilt / Sayı / Sayfa | 175 / 1 / – | DOI | 10.1016/j.bioorg.2026.109778 |
| Makale Linki | https://doi.org/10.1016/j.bioorg.2026.109778 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| Neurodegenerative diseases involve the convergence of cholinergic dysfunction, neuronal loss, and sustained neuroinflammatory responses, necessitating the development of multifunctional therapeutic agents. In this study, a series of novel thieno[3,2-d]pyrimidine–phenolic Mannich base hybrids were rationally designed, synthesized, and evaluated as dual cholinesterase inhibitors with neuroprotective and anti-neuroinflammatory potential. The synthesized compounds exhibited potent inhibition against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with inhibition constants in the low nanomolar range. Among them, compounds 5 and 9 emerged as the most active derivatives, displaying Ki values of 8.79 and 14.11 nM for AChE and 7.04 and 11.75 nM for BChE, surpassing the reference inhibitors tacrine and donepezil. Molecular docking and molecular dynamics simulations supported the … |
| Anahtar Kelimeler |
| Chlolinesterases | Neurodegeneration | Neuroinflammation | SH-SY5Y cells | Thieno[3,2-d]pyrimidine |
Science Direct
Targeting cholinergic dysfunction and neuroinflammation through rationally designed Thieno[3,2-d]pyrimidine hybrids
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 3 |
| Scopus | 4 |
| Google Scholar | 6 |