BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides

Bertini, Simone; Ghilardi, Elisa; Asso, Valentina; Granchi, Carlotta; Minutolo, Filippo; Pineschi, Mauro; Bussolo, Valeria Di; Bortolato, Andrea; Moro, Stefano

doi:10.1016/j.bmc.2010.09.032

Cited by 7 publications

(2 citation statements)

References 14 publications

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“…The following compounds have been reported previously: N -benzylprop-2-en-1-amine ( 1 ), N -(4-methoxybenzyl)prop-2-en-1-amine ( 2 ), 1-(4-benzhydrylpiperazin-1-yl)-3-(benzylamino)propan-2-ol ( 14) , and tert -butyl-dimethyl(2-(oxiran-2-yl)ethoxy)silane ( 18 ) …”

Section: Methodsmentioning

confidence: 99%

Design, Synthesis, and Biological Evaluation of 1-Benzylamino-2-hydroxyalkyl Derivatives as New Potential Disease-Modifying Multifunctional Anti-Alzheimer’s Agents

Panek

Więckowska

Jończyk

et al. 2018

ACS Chem. Neurosci.

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The multitarget approach is a promising paradigm in drug discovery, potentially leading to new treatment options for complex disorders, such as Alzheimer's disease. Herein, we present the discovery of a unique series of 1-benzylamino-2-hydroxyalkyl derivatives combining inhibitory activity against butyrylcholinesterase, β-secretase, β-amyloid, and tau protein aggregation, all related to mechanisms which underpin Alzheimer's disease. Notably, diphenylpropylamine derivative 10 showed balanced activity against both disease-modifying targets, inhibition of β-secretase (IC = 41.60 μM), inhibition of amyloid β aggregation (IC = 3.09 μM), inhibition of tau aggregation (55% at 10 μM); as well as against symptomatic targets, butyrylcholinesterase inhibition (IC = 7.22 μM). It might represent an encouraging starting point for development of multifunctional disease-modifying anti-Alzheimer's agents.

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Section: Methodsmentioning

confidence: 99%

Design, Synthesis, and Biological Evaluation of 1-Benzylamino-2-hydroxyalkyl Derivatives as New Potential Disease-Modifying Multifunctional Anti-Alzheimer’s Agents

Panek

Więckowska

Jończyk

et al. 2018

ACS Chem. Neurosci.

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“…Other strategies are investigated but they have not yet passed through clinical trials successfully or been commercialized for a general use. New types of cholinesterase inhibitors can be pointed out of which huperzine and its ZT-1 derivative can be introduced as drugs on a common principle (52,53) whereas other approaches like vaccination against tau and amyloid beta (54,55) or synthesis of new β secretase inhibitors (56,57) are other ways of pharmacologic treatments.…”

Section: Current Therapy and The Major Pathological Processes Relatedmentioning

confidence: 99%

Oxidative stress in Alzheimer disease as a target for therapy

Pohanka¹

2018

BLL

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In the recent time, neurodegenerative disorders like Alzheimer disease were recognized for their significant role in the current healthcare because of their growing incidence and costs for health insurance systems. Effective therapy is missing and even etiology of the diseases like Alzheimer disease is not deeply known. In the case of Alzheimer disease, it is probable that oxidative stress is at least a factor involved in the disease. Nevertheless, the current literature is controversial and ambiguous in this matter. This review is focused on mapping the role of oxidative stress as well as on a consideration that oxidative stress represents the pathway at which a therapeutic strategy can be aimed. This paper provides a survey of contemporary literature on oxidative stress in Alzheimer disease and discusses the opportunities for establishing a therapy based on interfering the stress (Fig. 5, Ref. 117).

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