Novel thiazole-piperazine derivatives as potential cholinesterase inhibitors
![Thumbnail](/xmlui/themes/Mirage2//images/restricted.png)
Göster/ Aç
Erişim
info:eu-repo/semantics/embargoedAccessTarih
2019Yazar
Demirayak, ŞerefŞahin, Zafer
Ertaş, Merve
Bülbül, Emre Fatih
Bender, Ceysu
Biltekin, Sevde Nur
Berk, Barkın
Sağlık, Begüm Nurpelin
Levent, Serkan
Yurttaş, Leyla
Üst veri
Tüm öğe kaydını gösterKünye
Demirayak, Ş., Şahin, Z., Ertaş, M., Bülbül, E. F., Bender, C., Biltekin, S. N. ... Yurttaş, L. (2019). Novel thiazole-piperazine derivatives as potential cholinesterase inhibitors. Journal of Heterocyclic Chemistry, 56(12), 3370-3386. https://doi.org/10.1002/jhet.3734Özet
Dementia is a cognitive disorder mostly associated with Alzheimer's disease (AD) in addition to being seen in many other diseases of the central nervous system (CNS). The limited number of drugs is not sufficient to provide adequate improvement to increase the quality of life of patients suffering from this symptom; therefore, all treatment options should be evaluated in detail. In this study, new molecules, [2-(4-(2/3/4-substituted phenyl)piperazin-1-yl)-4-phenylthiazol-5-yl][3/4-substituted phenyl]methanone derivatives (1-44), were obtained and analyzed in terms of their anticholinesterase activities. Kinetic mode and molecular interactions were also evaluated. An enzyme inhibition study was undertaken on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using the Ellman method. Maestro program was used in molecular modeling studies. Forty-four compounds were evaluated on AChE and BChE enzymes at 10(-3) and 10(-4) concentrations. The inhibition concentrations were calculated as 0.268 mu M to 2.104 mu M for six compounds (4, 5, 16, 27, 37, and 38) on AChE. Compound 5 including the 4-methoxy substituent (IC50: 0.268 mu M) and compound 38 containing the 4-methoxy and 3-methyl substituents (IC50: 0.286 mu M) showed the highest AChE inhibitory activity. They were further examined in terms of hydrogen bonding with Arg296 and Ar-Ar interaction with Trp286. The activity of compound 5 was also assessed in mixed-type kinetic mode.
WoS Q Kategorisi
Q3Scopus Q Kategorisi
Q3Kaynak
Journal of Heterocyclic ChemistryCilt
56Sayı
12Koleksiyonlar
- Makale Koleksiyonu [285]
- Scopus İndeksli Yayınlar Koleksiyonu [6620]
- WoS İndeksli Yayınlar Koleksiyonu [6696]