Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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3,4-Dihydrospiro[piperidine-4,2-(1H)quinoline] Derivatives as New Antioxidant Agents with Acetylcholinesterase Inhibitory Property

Author(s): Vladimir V. Kouznetsov, Leonor Y. Vargas Mendez, Amner Munoz Acevedo.

Abstract:

In vitro radical-cation scavenging capacity and anti-AChE activities of 19 piperidine derivatives, including dihydrospiro[ piperidine-4,2(1H)quinolines] 7-19 and their precursor 4-allyl-4-arylaminopiperidines 1-6 were reported. Their data of bioassays and calculated logP and TPSA parameters showed promising drug-like properties. The best radical scavenging compound (TEAC 1.73 ± 0.01), 6-methyl-3,4- dihydrospiro[piperidine-4,2(1H)quinoline] 8 showed IC50 value of 62.5 μM (20.0 μg/mL) using AChE assay.

Keywords: Antioxidant capacity, AChE inhibitory activity, Intramolecular Friedel-Crafts cyclization, Dihydrospiro[piperidine-4,2'(1'H)quinoline] derivatives, Multifunctional drug discovery, 4-allyl-4-arylaminopiperidines, AChE assay, Alzheimer's disease, AD, tacrine, rivas-tigmine, donepezil, galantamine, acetylcholine, hyperphosphory-lation, tacrine-ferullic hybrids, tacrine-melatonin, TMTHQ, Physostigmine, Trolox, Toluene, Allylmagnesium bromide, H-NMR, C-NMR, TPSA, BHT, 2,6-di-tert-butyl-4-methylphenol, BHA, 2-tert-butyl-4-hydroxyanisol, Trolox® Equivalent Antioxidant Capacity, TEAC, Ellman's reagent, DTNB, 5,5'-dithio-bis-2-nitrobenzoic acid, N-benzyl-6-methyl-3',4'-dihydrospiro[piperi-dine-4,2'(1'H)quinoline], N-benzyldihydrospiro[piperi-dine-4,2'(1'H)quinoline]

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Article Details

VOLUME: 7
ISSUE: 10
Year: 2010
Page: [710 - 715]
Pages: 6
DOI: 10.2174/1570180811007010710
Price: $58