TY - JOUR
T1 - Analysis of the antioxidant properties of differently substituted 2- and 3-indolyl carbohydrazides and related derivatives
AU - Hadjipavlou-Litina, Dimitra
AU - Samadi, Abdelouahid
AU - Unzeta, Mercedes
AU - Marco-Contelles, José
N1 - Funding Information:
JMC and MU thank MINECO for grant SAF2012-33304 , and EU ( COST Action CM-1103) for support. The authors gratefully acknowledge Dr. A. Leo and Biobyte Corp. 201 West 4th Street, Suite 204, Claremont, CA 91711, USA for free access to the C-QSAR program.
PY - 2013
Y1 - 2013
N2 - Herein, we report the antioxidant properties of some selected substituted 2-indolyl carbohydrazides (JL34, JL40, JL71, JL87, JL317, JL432, JL436), the substituted 3-indolyl carbohydrazide JL344, 3-(3-hydrazinylpropyl)-1H-indole (JL72) and 3-(1H-indol-3-yl)propanehydrazide (JL418), throughout the assessment of their antioxidative potential using different antioxidant assays such as DPPH, lipid peroxidation in the APPH, or the DMSO method. We conclude that these compounds are convenient templates for the design of useful drugs in to treat Alzheimer's disease (AD), a pathology characterized by extensive oxidative stress and inflammation, thus essentially affected by reactive oxygen species (ROS). Most of them are potent hydroxyl radical scavengers and inhibit in vitro lipid peroxidation. Compounds JL40 and JL432 presenting higher lipoxygenase inhibitory activity among the tested derivatives, were found to present a promising anti-inflammatory in vivo result, as well as antioxidant and LOX inhibitory profile. These results in combination to their known AChE/BuChE inhibitory activities led us to propose these indolyl carbohydrazides as new multifunctional compounds against AD.
AB - Herein, we report the antioxidant properties of some selected substituted 2-indolyl carbohydrazides (JL34, JL40, JL71, JL87, JL317, JL432, JL436), the substituted 3-indolyl carbohydrazide JL344, 3-(3-hydrazinylpropyl)-1H-indole (JL72) and 3-(1H-indol-3-yl)propanehydrazide (JL418), throughout the assessment of their antioxidative potential using different antioxidant assays such as DPPH, lipid peroxidation in the APPH, or the DMSO method. We conclude that these compounds are convenient templates for the design of useful drugs in to treat Alzheimer's disease (AD), a pathology characterized by extensive oxidative stress and inflammation, thus essentially affected by reactive oxygen species (ROS). Most of them are potent hydroxyl radical scavengers and inhibit in vitro lipid peroxidation. Compounds JL40 and JL432 presenting higher lipoxygenase inhibitory activity among the tested derivatives, were found to present a promising anti-inflammatory in vivo result, as well as antioxidant and LOX inhibitory profile. These results in combination to their known AChE/BuChE inhibitory activities led us to propose these indolyl carbohydrazides as new multifunctional compounds against AD.
KW - APPH
KW - Antioxidant
KW - DPPH
KW - Hydroxyl radicals
KW - LOX
KW - Lipid peroxidation
KW - ROS
KW - Substituted 2- and 3-indolyl carbohydrazides
KW - Superoxide anion radical (O)
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U2 - 10.1016/j.ejmech.2013.03.014
DO - 10.1016/j.ejmech.2013.03.014
M3 - Article
C2 - 23567956
AN - SCOPUS:84875959598
SN - 0223-5234
VL - 63
SP - 670
EP - 674
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -