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Synthesis and Evaluation of Neuroprotective α,β-Unsaturated Aldehyde Scavenger Histidyl-Containing Analogues of Carnosine
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2005
Year
Medicinal ChemistryPharmacological StudyBiochemistryMedicineNatural SciencesNeuroprotective αHistidyl-containing Carnosine AnaloguesNeuropharmacologyPharmacological AgentExperimental PharmacologyNeuroprotectionSynthetic ChemistryPharmacologyPharmaceutical Chemistry1,2-Diol MoietiesDrug DiscoverySh-sy5y Neuroblastoma CellsNatural Product Synthesis
The synthesis, scavenging activity, and cytoprotective profiles of histidyl-containing carnosine analogues bearing hydrazide or 1,2-diol moieties is reported. Some compounds have demonstrated higher aldehyde-sequestering efficiency than carnosine and were also efficient in protecting SH-SY5Y neuroblastoma cells and rat hippocampal neurons from 4-hydroxy-trans-2,3-nonenal (HNE)-mediated death. The cytoprotective efficacy of these compounds suggests their potential use as therapeutic agents for disorders that involve excessive membrane lipids peroxidation and HNE-mediated neuronal toxicity.
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