1240892-75-4Relevant academic research and scientific papers
Design, synthesis and biological activity of 1H-indene-2-carboxamides as multi-targeted anti-Alzheimer agents
Koca, Mehmet,Yerdelen, Kadir Ozden,Anil, Baris,Kasap, Zeynep,Sevindik, Handan,Ozyurek, Ibrahim,Gunesacar, Gulsen,Turkaydin, Kubra
, p. 13 - 23 (2016)
The aim of this study was to design new molecules and evaluate their anticholinesterase and amyloid beta (Aβ1–42) inhibition activities as multifunctional drug candidates for the treatment of Alzheimer’s disease (AD). A series of 5,6-dimethoxy-1H-indene-2-carboxamides (1–22) was synthesized; cholinesterase inhibitory activities of the compounds were measured according to Ellman’s colorimetric assay, while the thioflavin T assay was used for measuring the inhibition of Aβ1–42 aggregation. The results revealed that most compounds showed higher inhibitory activity against BuChE than AChE. Compounds 20 and 21 were found to be the most potent BuChE inhibitors with respective IC50 values of 1.08 and 1.09 μM. Compounds 16, 20, 21 and 22 exhibited remarkable inhibition of Aβ1–42 aggregation. Kinetic analysis showed that the most potent BuChE inhibitor (20) acted as a noncompetitive inhibitor. Docking studies suggested that inhibitor 20 displayed many potential hydrogen-bondings with the PAS of BuChE. These results suggest that compound 20 may be an especially promising multifunctional drug for the prevention and treatment of AD.
Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease
Yerdelen, Kadir Ozden,Koca, Mehmet,Anil, Baris,Sevindik, Handan,Kasap, Zeynep,Halici, Zekai,Turkaydin, Kubra,Gunesacar, Gulsen
supporting information, p. 5576 - 5582 (2015/11/17)
Amyloid beta (Aβ) and cholinesterase enzymes (AChE, BuChE) are important biological targets for the effective treatment of Alzheimer's disease. In this study, the aim was to synthesize new donepezil-like secondary amide compounds that display a potent inhibition of cholinesterases and Aβ with antioxidant and metal chelation abilities. All test compounds showed activities against both ChEs and β1-42 inhibition. The most encouraging compound, 20, is an AChE inhibitor with high anti-aggregation activity (55.3%). Based on the results, compound 20 may be a promising structure in further research for new anti-Alzheimer's agents.
Design and synthesis of brazilin-like compounds
Pan, Chengxue,Zeng, Xianghui,Guan, Yifu,Jiang, Xiangliu,Li, Liang,Zhang, Hongbin
supporting information; experimental part, p. 425 - 429 (2011/04/22)
A general and flexible synthetic route, which leads to the synthesis of brazilin-like compounds, was developed. The aza-brazilin derivatives show strong anticancer activities in MTT assay towards a number of human cancer cell lines including HT29, A549, HL60, and K562. Georg Thieme Verlag Stuttgart New York.
