Abstract
Alzheimer's Disease (AD) is a multifactorial and fatal neurodegenerative disorder affecting around 35 million people worldwide, which is characterized by decline of cholinergic function, deregulation of amyloid beta (Aβ) oligomers formation and Aβ fibril deposition. Multi-Target- Directed Ligands (MTDLs) have emerged as an original strategy for developing new therapeutic agents on AD. Multicomponent Reactions (MCRs) are a useful alternative to sequential multistep syntheses, allowing scaffold diversity and a rapid and easy access to biologically relevant compounds. The biological diversity of MCRs is very rich providing great possibilities for researchers interested in bioactive small molecular weight compounds. Since the MTDL strategy has been used to develop compounds endowed with the capacity to interact with different targets, versatile compound libraries may be obtained by MCRs according to the well established features of each target. Thus, either MTDLs or monotarget compounds have been developed by MCRs to address different factors implicated in AD. This work focuses on antioxidants, calcium channel modulators, both AChE and BuChE inhibitors, BACE1 inhibitors, and modulators of the nuclear factor (erythroid-derived 2)-like 2. First, we discuss the Biginelli reaction and its use for developing new interesting compounds for AD, followed by the contribution of Ugi reaction and, finally, the interest of other MCRs in the same topic.
Keywords: Alzheimer's Disease, Multicomponent reactions, Multitargeted compounds, Multi-target-Directed Ligands, Ugi reaction, Biginelli reaction.
Current Topics in Medicinal Chemistry
Title:Multicomponent Reactions for Multitargeted Compounds for Alzheimer`s Disease
Volume: 17 Issue: 31
Author(s): Lhassane Ismaili*Maria do Carmo Carreiras
Affiliation:
- Neurosciences Integratives et Cliniques EA 481, Laboratoire de Chimie Organique et Therapeutique, UFR SMP, 19 rue Ambroise Pare, Universite Bourgogne Franche-Comte, F25000 Besancon,France
Keywords: Alzheimer's Disease, Multicomponent reactions, Multitargeted compounds, Multi-target-Directed Ligands, Ugi reaction, Biginelli reaction.
Abstract: Alzheimer's Disease (AD) is a multifactorial and fatal neurodegenerative disorder affecting around 35 million people worldwide, which is characterized by decline of cholinergic function, deregulation of amyloid beta (Aβ) oligomers formation and Aβ fibril deposition. Multi-Target- Directed Ligands (MTDLs) have emerged as an original strategy for developing new therapeutic agents on AD. Multicomponent Reactions (MCRs) are a useful alternative to sequential multistep syntheses, allowing scaffold diversity and a rapid and easy access to biologically relevant compounds. The biological diversity of MCRs is very rich providing great possibilities for researchers interested in bioactive small molecular weight compounds. Since the MTDL strategy has been used to develop compounds endowed with the capacity to interact with different targets, versatile compound libraries may be obtained by MCRs according to the well established features of each target. Thus, either MTDLs or monotarget compounds have been developed by MCRs to address different factors implicated in AD. This work focuses on antioxidants, calcium channel modulators, both AChE and BuChE inhibitors, BACE1 inhibitors, and modulators of the nuclear factor (erythroid-derived 2)-like 2. First, we discuss the Biginelli reaction and its use for developing new interesting compounds for AD, followed by the contribution of Ugi reaction and, finally, the interest of other MCRs in the same topic.
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Cite this article as:
Ismaili Lhassane*, do Carmo Carreiras Maria , Multicomponent Reactions for Multitargeted Compounds for Alzheimer`s Disease, Current Topics in Medicinal Chemistry 2017; 17 (31) . https://dx.doi.org/10.2174/1568026618666180112155424
DOI https://dx.doi.org/10.2174/1568026618666180112155424 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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