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Synthesis of a second generation chroman/catechol hybrids and evaluation of their activity in protecting neuronal cells from oxidative stress-induced cell death

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Synthesis of a second generation chroman/catechol hybrids and evaluation of their activity in protecting neuronal cells from oxidative stress-induced cell death
Κουφάκη, Μαρία
Theodorou, Elissavet
Alexi, Xanthippi
Αλέξης, Μιχαήλ Ν.
Άρθρο σε επιστημονικό περιοδικό
2010-06-01
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.
OXFORD
Οργανική χημεία (EL)
Βιολογία (Γενικά) (EL)
Χημεία (Γενικά) (EL)
Φαρμακευτική (EL)
Biology (General) (EN)
Organic chemistry (EN)
Pharmacy and materia medica (EN)
Chemistry (General) (EN)
Oxidative stress
Neuronal damage
Bioisosterism
Catechol
Chroman
Chemistry, Medicinal
English
Pergamon
Bioorganic & Medicinal Chemistry
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© 2010 Elsevier Ltd. All rights reserved.
© 2010 Elsevier Ltd. All rights reserved. (EN)
National Hellenic Research Foundation (NHRF)
Helios - Repository of the National Hellenic Research Foundation (NHRF)



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