title: Analysis of the antioxidant properties of differently substituted 2- and 3-indolyl carbohydrazides and related derivatives.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124, Greece. hadjipav@pharm.auth.gr
authors.forename: Dimitra
authors.initials: D
authors.lastname: Hadjipavlou-Litina
authors.forename: Abdelouahid
authors.initials: A
authors.lastname: Samadi
authors.forename: Mercedes
authors.initials: M
authors.lastname: Unzeta
authors.forename: José
authors.initials: J
authors.lastname: Marco-Contelles
mesh_terms: D000544:Alzheimer Disease / Q000378:metabolism / Q000517:prevention & control; D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D055162:Biocatalysis / Q000187:drug effects; D001713:Biphenyl Compounds / Q000378:metabolism; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control; D005260:Female; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006834:Hydrazines / Q000737:chemistry / Q000494:pharmacology*; D015227:Lipid Peroxidation / Q000187:drug effects*; D008084:Lipoxygenase / Q000378:metabolism; D008297:Male; D015394:Molecular Structure; D010084:Oxidation-Reduction / Q000187:drug effects; D010851:Picrates / Q000378:metabolism; D051381:Rats; D011916:Rats, Inbred F344; D013329:Structure-Activity Relationship
chemical_list: D000975:Antioxidants; D001713:Biphenyl Compounds; D016166:Free Radical Scavengers; D006834:Hydrazines; D010851:Picrates; D002351:Carrageenan; C004931:1,1-diphenyl-2-picrylhydrazyl; D008084:Lipoxygenase; C019289:carbohydrazide