RT Journal Article
T1 Improving the Efficacy of Quinolylnitrones for Ischemic Stroke Therapy, QN4 and QN15 as New Neuroprotective Agents after Oxygen–Glucose Deprivation/Reoxygenation-Induced Neuronal Injury
A1 Fernández López, Israel
A1 Alonso Gómez, José Miguel
A1 Escobar Peso, Alejandro
A1 Alcázar, Alberto
A1 Marco Contelles, José
AB In our search for new neuroprotective agents for stroke therapy to improve the pharmacological profile of the compound quinolylnitrone QN23, we have prepared and studied sixteen new related and easily available quinolylnitrones. As a result, we have identified compounds QN4 and QN15 as promising candidates showing high neuroprotection power in a cellular experimental model of ischemia. Even though they were found to be less active than our current lead compound QN23,QN4 and QN15 provide an improved potency and, particularly for QN4, an expanded range of tolerability and improved solubility compared to the parent compound. A computational DFT-based analysis has been carried out to understand the antioxidant power of quinolylnitrones QN23, QN4and QN15. Altogether, these results show that subtle, simple modifications of the quinolylnitrone scaffold are tolerated, providing high neuroprotective activity and optimization of the pharmacological potency required for an improved design and future drug developments in the field.
PB MDPI
SN 1424-8247
YR 2022
FD 2022-11-07
LK https://hdl.handle.net/20.500.14352/88175
UL https://hdl.handle.net/20.500.14352/88175
LA eng
NO Alonso, José M, Escobar Peso, Alejandro, Fernández, Israel, Álcazar, Alberto, Marco Contelles, José. Improving the Efficacy of Quinolylnitrones for Ischemic Stroke Therapy, QN4 and QN15 as New Neuroprotective Agents after Oxygen–Glucose Deprivation/Reoxygenation-Induced Neuronal Injury. Pharmaceuticals, 2022 15(11): 1363-84
DS Docta Complutense
RD 21 abr 2025