Synthesis of Novel Aryloxyethylamine Derivatives and Evaluation of Their in Vitro and in Vivo Neuroprotective Activities.

Synthesis of Novel Aryloxyethylamine Derivatives and Evaluation of Their in Vitro and in Vivo Neuroprotective Activities. Chem Biodivers. 2020 Jun 24;: Authors: Zhong Y, Gao Y, Xu Y, Qi C, Wu B Abstract A series of aryloxyacetamine derivatives W1 - W37 were designed, synthesized and evaluated for their biological activity. Their structures were confirmed by 1 H-NMR, 13 C-NMR, and HR-ESI-MS. The preliminary screening of neuroprotection of compounds in vitro was detected by MTT, and the anti-ischaemic activity in vivo was tested using bilateral common carotid artery occlusion in Kunming Mice. Most of these compounds showed potent neuroprotective effects against the glutamate-induced cell death in differentiated rat pheochromocytoma cells (PC12 cells), especially for W1 , W7 , W16 , W26 , W28 , W29 and W30 , which exhibited potential protection of PC12 cells at three doses (0.1, 1.0, 10 µM). Compounds W1 , W4 , W7 and W26 possessed the significant prolongation of the survival time of mice subjected to acute cerebral ischemia and decrease the mortality rate at all five doses tested (200, 100, 50, 25, 12.5 mg/kg) and exhibited potent neuroprotective activity. In particular, W1 , W7 and W26 possessed outstanding neuroprotective activities in vitro and in vivo , these compounds can be lead compounds for further discovery of neuroprotective agents for treating cerebral ischemic stroke. Basic structure-activity relationships are also present...
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research