期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 37, 期 1, 页码 2660-2678出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2022.2126464
关键词
Indole; Alzheimer's disease; inflammation; AChE; BuChE
资金
- Beni-Suef University Performance Development Center, Support and Project Finance office [BSU-CP7-19004]
A novel series of indole-based compounds were designed and synthesised as anti-Alzheimer's and anti-neuroinflammatory agents. Some of the designed compounds showed selectivity for AChE and BuChE inhibitory activities, while others exerted dual inhibitory activities. Additionally, certain compounds demonstrated the ability to inhibit self-induced A beta amyloid aggregation.
A novel series of indole-based compounds was designed, synthesised, and evaluated as anti-Alzheimer's and anti-neuroinflammatory agents. The designed compounds were in vitro evaluated for their AChE and BuChE inhibitory activities. The obtained results revealed that compound 3c had higher selectivity for AChE than BuChE, while, 4a, 4b, and 4d showed selectivity for BuChE over AChE. Compounds 5b, 6b, 7c, and 10b exerted dual AChE/BuChE inhibitory activities at nanomolar range. Compounds 5b and 6b had the ability to inhibit the self-induced A beta amyloid aggregation. Different anti-inflammatory mediators (NO, COX-2, IL-1 beta, and TNF-alpha) were assessed for compounds 5b and 6b. Cytotoxic effect of 5b and 6b against human neuroblastoma (SH-SY5Y) and normal hepatic (THLE2) cell lines was screened in vitro. Molecular docking study inside rhAChE and hBuChE active sites, drug-likeness, and ADMET prediction were performed.
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