Recent development of multifunctional agents as potential drug candidates for the treatment of Alzheimer's disease

N Guzior, A Wieckowska, D Panek… - Current medicinal …, 2015 - ingentaconnect.com
Alzheimer's disease (AD) is a complex and progressive neurodegenerative disorder. The
available therapy is limited to the symptomatic treatment and its efficacy remains …

Development of phenothiazine hybrids with potential medicinal interest: a review

MC Posso, FC Domingues, S Ferreira, S Silvestre - Molecules, 2022 - mdpi.com
The molecular hybridization approach has been used to develop compounds with improved
efficacy by combining two or more pharmacophores of bioactive scaffolds. In this context …

Blood–brain barrier models and their relevance for a successful development of CNS drug delivery systems: a review

J Bicker, G Alves, A Fortuna, A Falcão - European Journal of Pharmaceutics …, 2014 - Elsevier
During the research and development of new drugs directed at the central nervous system,
there is a considerable attrition rate caused by their hampered access to the brain by the …

New Tacrine–4-Oxo-4H-chromene Hybrids as Multifunctional Agents for the Treatment of Alzheimer's Disease, with Cholinergic, Antioxidant, and β-Amyloid …

MI Fernández-Bachiller, C Pérez… - Journal of medicinal …, 2012 - ACS Publications
By using fragments endowed with interesting and complementary properties for the
treatment of Alzheimer's disease (AD), a new family of tacrine–4-oxo-4 H-chromene hybrids …

Multi-target-directed ligands and other therapeutic strategies in the search of a real solution for Alzheimer's disease

A Agis-Torres, M Sollhuber… - Current …, 2014 - ingentaconnect.com
The lack of an adequate therapy for Alzheimer's Disease (AD) contributes greatly to the
continuous growing amount of papers and reviews, reflecting the important efforts made by …

Discovery of the first dual GSK3β inhibitor/Nrf2 inducer. A new multitarget therapeutic strategy for Alzheimer's disease

I Gameiro, P Michalska, G Tenti, Á Cores, I Buendia… - Scientific reports, 2017 - nature.com
The formation of neurofibrillary tangles (NFTs), oxidative stress and neuroinflammation have
emerged as key targets for the treatment of Alzheimer's disease (AD), the most prevalent …

Investigating 1, 2, 3, 4, 5, 6-hexahydroazepino [4, 3-b] indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for …

R Purgatorio, M de Candia, M Catto, A Carrieri… - European Journal of …, 2019 - Elsevier
Due to the role of butyrylcholinesterase (BChE) in acetylcholine hydrolysis in the late stages
of the Alzheimer's disease (AD), inhibitors of butyrylcholinesterase (BChE) have been …

Novel Tacrine‐Grafted Ugi Adducts as Multipotent Anti‐Alzheimer Drugs: A Synthetic Renewal in Tacrine–Ferulic Acid Hybrids

M Benchekroun, M Bartolini, J Egea, A Romero… - …, 2015 - Wiley Online Library
Herein we describe the design, multicomponent synthesis, and biological, molecular
modeling and ADMET studies, as well as in vitro PAMPA‐blood–brain barrier (BBB) analysis …

Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9, 10, 11, 12-tetrahydro-7H-benzo [7, 8] chromeno [2, 3-b] quinolin-8-amines as potential …

E Maalej, F Chabchoub, MJ Oset-Gasque… - European journal of …, 2012 - Elsevier
The synthesis, pharmacological analysis and molecular modeling of the readily available
racemic tacrine analogs 21–30, bearing the 7-aryl-9, 10, 11, 12-tetrahydro-7H-benzo [7, 8] …

New azepino [4, 3-b] indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced …

M De Candia, G Zaetta, N Denora, D Tricarico… - European journal of …, 2017 - Elsevier
Abstract Several 6-substituted 3, 4, 5, 6-tetrahydroazepino [4, 3-b] indol-1 (2H)-one (THAI)
derivatives were synthesized and evaluated for their activity as cholinesterase (ChE) …