Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists

Publication date: Available online 19 May 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Milad Espahbodinia, Roberta Ettari, Wei Wen, Andrew Wu, Yu-Chuan Shen, Li Niu, Silvana Grasso, Maria Zappalà
In this work, we designed and synthesized novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists, with the aim that this heterocycle could establish favourable interactions with a putative binding pocket of the receptor, like the thiadiazole nucleus of GYKI 47409 does. Within this investigation, we identified some active molecules and, among these 2,3-benzodiazepines, 4c showed a much improved inhibitory potency as compared with unsubstituted 2,3-benzodiazepines.

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