Synthesis and evaluation of novel xanthene-based thiazoles as potential antidiabetic agents
Yükleniyor...
Tarih
2022
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
WILEY-V C H VERLAG GMBH
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
A series of xanthene-based thiazoles was synthesized and characterized by different scpectroscopic methods, i.e. Proton nuclear magnetic resonance (H-1 NMR), carbon nuclear magnetic resonance (C-13 NMR), infrared spectroscopy, carbon hydrogen nitrogen analysis, and X-ray crystallography. The inhibition potencies of 18 newly synthesized thiazole derivatives were investigated on the activities of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), alpha-amylase (alpha-Amy), and alpha-glycosidase (alpha-Gly) enzymes in accordance with their antidiabetic and anticholinesterase ability. The synthesized compounds have the highest inhibition potential against the enzymes at low nanomolar concentrations. Among the 18 newly synthesized molecules, 3b and 3p were superior to the known commercial inhibitors of the enzymes and have a much more effective inhibitory potential, with IC50: 2.37 and 1.07 nM for AChE, 0.98 and 0.59 nM for BChE, 56.47 and 61.34 nM for alpha-Gly, and 152.48 and 124.84 nM for alpha-Amy, respectively. Finally, the optimized 18 compounds were subjected to molecular docking to describe the interaction between thiazole derivatives and AChE, BChE, alpha-Amy, and alpha-Gly enzymes in which important interactions were monitored with amino acid residues of each target enzyme.
Açıklama
Anahtar Kelimeler
Alpha-amylase, Alpha-glycosidase, Cholinesterase, Molecular Docking, Thiazoline, Xanthene
Kaynak
ARCHIV DER PHARMAZIE
WoS Q Değeri
Q2
Scopus Q Değeri
N/A
Cilt
Sayı
Künye
Naseem, S., Shafiq, Z., Taslimi, P., Hussain, S., Taskin‐Tok, T., Kisa, D., ... & El‐Gokha, A. (2022). Synthesis and evaluation of novel xanthene‐based thiazoles as potential antidiabetic agents. Archiv der Pharmazie, e2200356.
