Design,Synthesis And Biological Activities Of Novel Neuroprotective Agents For Acute Ischemic Stroke

Acute ischemic stroke is the major cause of disability.Except for Edaravone,many pharmacological treatments by means of so-called neuroprotective drugs such as glutamate receptor antagonists and Ca and/or Na channel blockers have been tried;however,they have not been successful in improving clinical outcome in patients.In order to explore new neuroprotective compounds,44 novel target compounds have been designed and synthesized by using computer-aided drug design,their structures were confirmed by ¹H NMR,¹³C NMR and HRMS.The biological test and preliminary pharmacological screening of all the compounds showed that compound WBWJ-33 and WBWJ-35 exhibit potent neuroprotective effects.Further bioassay and structural optimizing of these derivatives as neuroprotective agents are in progress.Besides,we have do something with codurgs by combinating Edaravone and selective antagonist of NR2B subunit in a simple compound.A novel target compound has been synthesized.The related biological test and pharmacological test are also in progress.