{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Herrera-Arozamena C"],"funding":["Agencia Estatal de Investigación, Ministerio de Ciencia, Innovación y Universidades","Sociedad Española de Química Terapéutica","Consejo Superior de Investigaciones Científicas","Instituto de Salud Carlos III","Fundación Teófilo Hernando","European Structural Funds","General Council for Research and Innovation of the Community of Madrid","Ministerio de Educación - Gobierno de España","European Regional Development Fund"],"pagination":["4727-4751"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8958504"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["65(6)"],"pubmed_abstract":["By replacing a phenolic ring of (<i>E</i>)-resveratrol with an 1,3,4-oxadiazol-2(3<i>H</i>)-one heterocycle, new resveratrol-based multitarget-directed ligands (MTDLs) were obtained. They were evaluated in several assays related to oxidative stress and inflammation (monoamine oxidases, nuclear erythroid 2-related factor, quinone reductase-2, and oxygen radical trapping) and then in experiments of increasing complexity (neurogenic properties and neuroprotection <i>vs</i> okadaic acid). 5-[(<i>E</i>)-2-(4-Methoxyphenyl)ethenyl]-3-(prop-2-yn-1-yl)-1,3,4-oxadiazol-2(3<i>H</i>)-one (<b>4e</b>) showed a well-balanced MTDL profile: cellular activation of the NRF2-ARE pathway (CD = 9.83 μM), selective inhibition of both hMAO-B and QR2 (IC<sub>50</sub>s = 8.05 and 0.57 μM), and the best ability to "],"journal":["Journal of medicinal chemistry"],"pubmed_title":["Resveratrol-Based MTDLs to Stimulate Defensive and Regenerative Pathways and Block Early Events in Neurodegenerative Cascades."],"pmcid":["PMC8958504"],"funding_grant_id":["RTI2018-095793-B-I00","PIE-202080I026","FPU13/03737","FPU18/00630","PIE-202080E118","PI17/01700","SAF2015-64948-C2-1-R","FPU16/01704","RTI2018-093955-B-C21","B2017/BMD-3827 - NRF24ADCM","FPU15/03269","PID2021-122650OB-I00","FPUEST17/00233"],"pubmed_authors":["Michalska P","Estrada-Valencia M","Sastre ED","Duarte P","Perez-Castillo A","Lopez MG","Lopez-Caballero P","Fernandez-Mendivil C","Herrera-Arozamena C","Perez C","Lombardia J","Leon R","Senar S","Rodriguez-Franco MI","Morales-Garcia JA"],"additional_accession":[]},"is_claimable":false,"name":"Resveratrol-Based MTDLs to Stimulate Defensive and Regenerative Pathways and Block Early Events in Neurodegenerative Cascades.","description":"By replacing a phenolic ring of (<i>E</i>)-resveratrol with an 1,3,4-oxadiazol-2(3<i>H</i>)-one heterocycle, new resveratrol-based multitarget-directed ligands (MTDLs) were obtained. They were evaluated in several assays related to oxidative stress and inflammation (monoamine oxidases, nuclear erythroid 2-related factor, quinone reductase-2, and oxygen radical trapping) and then in experiments of increasing complexity (neurogenic properties and neuroprotection <i>vs</i> okadaic acid). 5-[(<i>E</i>)-2-(4-Methoxyphenyl)ethenyl]-3-(prop-2-yn-1-yl)-1,3,4-oxadiazol-2(3<i>H</i>)-one (<b>4e</b>) showed a well-balanced MTDL profile: cellular activation of the NRF2-ARE pathway (CD = 9.83 μM), selective inhibition of both hMAO-B and QR2 (IC<sub>50</sub>s = 8.05 and 0.57 μM), and the best ability to ","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Mar","modification":"2026-05-31T06:03:48.81Z","creation":"2025-04-20T00:20:38.193Z"},"accession":"S-EPMC8958504","cross_references":{"pubmed":["35245051"],"doi":["10.1021/acs.jmedchem.1c01883"]}}