Κουφάκη, ΜαρίαTheodorou, ElissavetAlexi, XanthippiΑλέξης, Μιχαήλ Ν.A new generation of chroman/catechol hybrids bearing heterocyclic five-membered rings, such as 1,2, 4-oxadiazole 1,3,4-oxadiazole, 1,2,3-triazole, tetrazole and isoxazole, were designed and synthesized. The activity of the new derivatives against oxidative stress induced neuronal damage, was evaluated using glutamate-challenged hippocampal HT22 cells. Compound 3 in which a 3,4-dimethoxyphenyl moiety, is directly attached to the 1,2,4-oxadiazole ring was the most active among the 2-substituted chroman analogues, with EC(50) = 254 +/- 65 nM. Concerning the 5-subtituted chroman analogues, isoxazole derivative 29 exhibited the strongest activity (EC(50) = 245 +/- 38 nM). However, 29 was cytotoxic at concentrations higher than 1 mu M, while the triazole analogue 24 (EC(50) = 801 +/- 229 nM), was non-toxic at all concentrations tested.OXFORD3898-3909Adobe PDF10.1016/j.bmc.2010.04.042https://hdl.handle.net/10442/122700968-0896engPergamon© 2010 Elsevier Ltd. All rights reserved.© 2010 Elsevier Ltd. All rights reserved.Bioorganic & Medicinal ChemistryOxidative stressNeuronal damageBioisosterismCatecholChromanChemistry, MedicinalSynthesis of a second generation chroman/catechol hybrids and evaluation of their activity in protecting neuronal cells from oxidative stress-induced cell deathΆρθρο σε επιστημονικό περιοδικό2010-06-01Δημοσίευση σε περιοδικόPublication in journalΟργανική χημείαOrganic Chemistryisi - Chemistry, Organic includes resources that focus on synthetic and natural organic compounds their synthesis, structure, properties, and reactivity. Research on hydrocarbons, a major area of organic chemistry, is included in this category.Φαρμακευτική χημείαMedicinal chemistryisi - Chemistry, Medicinal includes resources emphasizing the isolation and study of substances with therapeutic potential. Topics of interest are quantitative structure-function relationships, structural characterization and organic syntheses of naturally occurring compounds, and chemical and analytical techniques used in rational drug design. See also the PHARMACOLOGY & PHARMACY category.Φαρμακολογία και ΦαρμακευτικήPharmacology and Pharmacyisi - Pharmacology & Pharmacy covers resources on the discovery and testing of bioactive substances, including animal research, clinical experience, delivery systems, and dispensing of drugs. This category also includes resources on the biochemistry, metabolism, and toxic or adverse effects of drugs.ΒιολογίαBiological sciencesFrascati 42Επιστημονικό άρθροScientific articleΕθνικό Ίδρυμα Ερευνών (ΕΙΕ)Greek Aggregator OpenArchives.gr | National Documentation Centre (EKT)