SYNTHESIS OF BENZIMIDAZOLE-SUGAR DERIVATIVES: A POTENTIAL TREATMENT FOR ALZHEIMER'S DISEASE

被引:1
作者
Yuksekdanaci, Seda [1 ]
Astley, Demet [2 ]
Senturk, Murat [3 ]
机构
[1] Usak Univ, Dept Occupat Hlth & Safety, Fac Hlth Sci, Usak, Turkiye
[2] Ege Univ, Dept Chem, Fac Sci, Izmir, Turkiye
[3] Agri Ibrahim Cecen Univ, Dept Biochem, Fac Pharm, Agri, Turkiye
来源
STUDIA UNIVERSITATIS BABES-BOLYAI CHEMIA | 2023年 / 68卷 / 04期
关键词
Benzimidazole; amino acid; glycosyl thiourea; carbonic anhydrase; cholinesterase; CARBONIC-ANHYDRASE II; BIOLOGICAL EVALUATION; INHIBITORY PROPERTIES; ISOZYMES I; PROTEIN; ACETYLCHOLINESTERASE; CHOLINESTERASES; DOCKING; BINDING;
D O I
10.24193/subbchem.2023.4.08
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In this study, a new series of chiral benzimidazole-glycosyl thiourea derivatives (5-10) were synthesized and evaluated for their inhibitory effects against hCA I, hCA II, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The structures of the benzimidazole-glycosyl thiourea compounds were determined by FTIR, 1H-NMR, 13C-NMR and elemental analysis. The KI values for the CA isoenzymes of the synthesized materials ranged from 6.03 to 42.98 nM. KI values for cholinesterase enzymes were shown to be between 5.32 and 39.14 nM. It was observed that compound 10 is the best hCA I inhibitor (KI:6.03 nM), compund 9 is the best hCAII inhibitor (KI:17.29 nM) and compound 8 is the best AChE (KI:5.32 nM) and the best BChE (KI:18.73 nM) inhibitor.
引用
收藏
页码:111 / 126
页数:16
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