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Cholinesterase inhibitory activity of highly functionalized fluorinated spiropyrrolidine heterocyclic hybrids

机译:高官能化氟化螺吡咯烷杂交物的胆碱酯酶抑制活性

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摘要

Two series of dimethoxyindanone imbedded novel fluorinated spiropyrrolidine heterocyclic hybrids were synthesized employing two different less explored azomethine ylides and were measured for their efficiency as inhibitors for Alzheimer’s disease. Among the spiropyrrolidine heterocyclic hybrids, the indole based fluorinated compound with a methoxy substituent at the meta- position of the aryl ring exhibited the utmost potent AChE and BChE inhibitory activities with an IC50 of 1.97 ± 0.19 µM and 7.08 ± 0.20 µM respectively. The plausible mechanism of inhibition on ChE receptors was unveiled via molecular docking studies.
机译:两种系列二甲氧基吲哚酮嵌入的新型氟化螺吡咯烷杂交杂交物合成使用两种不同较少探索的氮杂物棉花,以效率为Alzheimer疾病的抑制剂。在螺吡咯烷杂交杂交物中,芳族芳环的元定位的吲哚基氟化化合物具有甲氧基取代基的最大有效疼痛和BCHE抑制活性,IC50分别为1.97±0.19μm和7.08±0.20μm。通过分子对接研究推出了Che受体上抑制的可粘附机制。

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