Away from Flatness: Unprecedented Nitrogen-Bridged Cyclopenta[a]indene Derivatives as Novel Anti-Alzheimer Multitarget Agents

AA Titov, MS Kobzev, M Catto, M Candia… - ACS Chemical …, 2021 - ACS Publications
Nature-inspired, bridged polycyclic molecules share low similarity with currently available
drugs, containing preferentially planar and/or achiral moieties. This “Escape from Flatland” …

Targeting neuronal calcium channels and GSK3β for Alzheimer's disease with naturally-inspired Diels-Alder adducts

A Bisi, A Feoli, A Trezza, L Viejo, F Formaggio… - Bioorganic …, 2022 - Elsevier
The complexity of neurodegenerative diseases, among which Alzheimer's disease plays a
pivotal role, poses one of the tough therapeutic challenges of present time. In this …

Design, synthesis and multitarget biological profiling of second-generation anti-Alzheimer rhein–huprine hybrids

FJ Pérez-Areales, N Betari, A Viayna… - Future Medicinal …, 2017 - Future Science
Aim: Simultaneous modulation of several key targets of the pathological network of
Alzheimer's disease (AD) is being increasingly pursued as a promising option to fill the …

Direct Access to Quinone-Fused 5-Substituted-1, 4-Benzodiazepine Scaffolds from Azidoquinones with/without [1, 2]-Azide-Nitrogen Migration: Mechanistic Insights

A Krishnan, S Kamaraj - The Journal of Organic Chemistry, 2023 - ACS Publications
Seven-membered nitrogen heterocycles have a strong influence in drug discovery due to
their inherent 3D character, which allows the ability to explore a vast conformational space …

Navigating the chemical space of multitarget-directed ligands: from hybrids to fragments in Alzheimer's disease

F Prati, A Cavalli, ML Bolognesi - Molecules, 2016 - mdpi.com
Multitarget drug discovery is one of the hottest topics and most active fields in the search for
new molecules against Alzheimer's disease (AD). Over the last 20 years, many promising …

A focused library of psychotropic analogues with neuroprotective and neuroregenerative potential

E Uliassi, LE Peña-Altamira, AV Morales… - ACS Chemical …, 2018 - ACS Publications
Overcoming the lack of effective treatments and the continuous clinical trial failures in
neurodegenerative drug discovery might require a shift from the prevailing paradigm …

Exploring the multi–target neuroprotective chemical space of benzofuran scaffolds: A new strategy in drug development for Alzheimer's disease

JR Cabrera-Pardo, J Fuentealba, J Gavilán… - Frontiers in …, 2020 - frontiersin.org
Alzheimer's disease (AD) is an irreversible and progressive neurodegenerative disorder that
slowly destroys memory. The precise mechanism of AD is still not entirely understood and …

Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents

E Viayna, I Sola, M Bartolini, A De Simone… - Journal of Medicinal …, 2014 - ACS Publications
We have synthesized a family of rhein–huprine hybrids to hit several key targets for
Alzheimer's disease. Biological screening performed in vitro and in Escherichia coli cells …

Polycyclic cage structures as lipophilic scaffolds for neuroactive drugs

J Joubert, WJ Geldenhuys, CJ Van der Schyf… - …, 2012 - Wiley Online Library
Polycyclic cage scaffolds have been successfully used in the development of numerous lead
compounds demonstrating activity in the central nervous system (CNS). Several …

Tricyclic challenges: synthetic approaches toward dodecahydrocyclopenta [a] indenes

M Krebs, M Kalinowski, W Frey, B Claasen, A Baro… - Tetrahedron, 2013 - Elsevier
Abstract Tetrahydrospiro [1, 3-dioxolane-2, 1′-pentalen]-4′-ones were stereoselectively
converted to either (cis, anti, cis)-or (cis, syn)-linear dodecahydrocyclopenta [a] indene …