New Mannich-type arylidenerhodanines as potent inhibitors of AChE and BChE: synthesis, biological evaluation, cytotoxicity and molecular modeling
Yazarlar (6)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Dr. Öğr. Üyesi Orhan ULUÇAY Kafkas Üniversitesi, Türkiye
Mubashır Ameen Bahauddin Zakariya University, Pakistan
Zahıd Shafıq
Bahauddin Zakariya University, Pakistan
Bahauddin Zakariya University, Pakistan
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Rsc Advances (Q2) | ||
| Dergi ISSN | 2046-2069 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 12-2025 |
| Cilt / Sayı / Sayfa | 15 / 58 / 50186–50205 | DOI | 10.1039/d5ra07416a |
| Makale Linki | https://doi.org/10.1039/d5ra07416a | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| Alzheimer's disease (AD) is a neurodegenerative disorder with a gradual increase in severity. The underlying cause of the disease is the dysfunction of cholinergic neurotransmission affecting mainly the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Within the context of the present research, a new group of 3,5-disubstituted rhodanine derivatives containing tertiary amine groups has been prepared and their potency in the inhibition of AChE and BChE was assessed. Enzymatic assays demonstrated that compounds 6 and 11 exhibited exceptional inhibitory potency, with Ki values of 13.61 nM and 12.70 nM against AChE, and 10.44 nM and 25.11 nM against BChE, respectively, surpassing the reference inhibitors tacrine (145.21 nM for AChE and 169.54 nM for BChE) and donepezil (67.41 nM for AChE and 62.44 nM for BChE). Cytotoxicity studies confirmed minimal toxicity in human … |
| Anahtar Kelimeler |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 12 |
| Scopus | 12 |
| Google Scholar | 13 |