Polyphosphoric acid-promoted one-pot synthesis and neuroprotective effects of flavanones against NMDA-induced injury in PC12 cells

We report herein an efficient polyphosphoric acid (PPA) promoted one-pot protocol for the synthesis of flavanone derivatives from 2-hydroxyacetophenones and benzaldehydes. A variety of flavanones were produced in moderate to excellent yields and evaluated for their neuroprotective effects against N-...

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Detalles Bibliográficos
Autores principales: Wang, Enhua, Yang, Lishou, Yang, Qian, Yang, Fanghong, Luo, Ji, Gan, Menglan, Wang, Xue, Song, Shanmin, Lei, Yang, Yang, Xiaosheng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2022
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9528730/
https://www.ncbi.nlm.nih.gov/pubmed/36320275
http://dx.doi.org/10.1039/d2ra03562f
Descripción
Sumario:We report herein an efficient polyphosphoric acid (PPA) promoted one-pot protocol for the synthesis of flavanone derivatives from 2-hydroxyacetophenones and benzaldehydes. A variety of flavanones were produced in moderate to excellent yields and evaluated for their neuroprotective effects against N-methyl-d-aspartate (NMDA)-induced excitotoxicity in PC12 cells. Derivatives bearing electron-donating groups exhibited better neuroprotective activity. Compound 3m demonstrated the best protective potency and reversed the intracellular calcium (Ca(2+)) influx caused by NMDA, suggesting that flavanones protected the PC12 cells against NMDA-induced neurotoxicity via inhibition of Ca(2+) overload.

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