Multitarget‐directed therapeutics: (Urea/thiourea)2 derivatives of diverse heterocyclic‐Lys conjugates
Sign Up to like & getrecommendations! Published in 2021 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202000468
Abstract: The synthesis of a new small library of molecules containing bis‐urea/thiourea pendants in lysine conjugated to three different heterocycles is described. The heterocycles used in this study have benzisoxazole/piperazine/piperidine units. After a detailed antimicrobial, antioxidant,… read more here.
Keywords: directed therapeutics; thiourea derivatives; urea thiourea; therapeutics urea ... See more keywords
Dimeric Tacrine(10)-hupyridone as a Multitarget-Directed Ligand To Treat Alzheimer's Disease.
Sign Up to like & getrecommendations! Published in 2021 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.1c00182
Abstract: Alzheimer's disease (AD) is a neurodegenerative disorder with multiple pathological features. Therefore, a multitarget-directed ligands (MTDLs) strategy has been developed to treat AD. We have previously designed and synthesized dimeric tacrine(10)-hupyridone (A10E), a novel tacrine… read more here.
Keywords: alzheimer disease; a10e could; dimeric tacrine; a10e ... See more keywords
Design, Synthesis, and Pharmacological Evaluation of N-Propargylated Diphenylpyrimidines as Multitarget Directed Ligands for the Treatment of Alzheimer's Disease.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.2c00132
Abstract: Alzheimer's disease (AD), a multifactorial complex neural disorder, is categorized with progressive memory loss and cognitive impairment as main clinical features. The multitarget directed ligand (MTDL) strategy is explored for the treatment of multifactorial diseases… read more here.
Keywords: series; alzheimer disease; synthesis; treatment ... See more keywords
Novel Vilazodone-Tacrine Hybrids as Potential Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease Accompanied with Depression: Design, Synthesis, and Biological Evaluation.
Sign Up to like & getrecommendations! Published in 2017 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.7b00259
Abstract: Depression is one of the most frequent psychiatric complications of Alzheimer's disease (AD), affecting up to 50% of the patients. A novel series of hybrid molecules were designed and synthesized by combining the pharmacophoric features… read more here.
Keywords: potential multitarget; vilazodone tacrine; depression; alzheimer disease ... See more keywords
Merged Tacrine-Based, Multitarget-Directed Acetylcholinesterase Inhibitors 2015–Present: Synthesis and Biological Activity
Sign Up to like & getrecommendations! Published in 2020 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms21175965
Abstract: Acetylcholinesterase is an important biochemical enzyme in that it controls acetylcholine-mediated neuronal transmission in the central nervous system, contains a unique structure with two binding sites connected by a gorge region, and it has historically… read more here.
Keywords: directed acetylcholinesterase; multitarget directed; activity; acetylcholinesterase inhibitors ... See more keywords
Effects of Linkers and Substitutions on Multitarget Directed Ligands for Alzheimer’s Diseases: Emerging Paradigms and Strategies
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23116085
Abstract: Alzheimer’s disease (AD) is multifactorial, progressive and the most predominant cause of cognitive impairment and dementia worldwide. The current “one-drug, one-target” approach provides only symptomatic relief to the condition but is unable to cure the… read more here.
Keywords: linkers substitutions; ligands alzheimer; directed ligands; effects linkers ... See more keywords
Benzophenone Derivatives with Histamine H3 Receptor Affinity and Cholinesterase Inhibitory Potency as Multitarget-Directed Ligands for Possible Therapy of Alzheimer’s Disease
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules28010238
Abstract: The multitarget-directed ligands demonstrating affinity to histamine H3 receptor and additional cholinesterase inhibitory potency represent a promising strategy for research into the effective treatment of Alzheimer’s disease. In this study, a novel series of benzophenone… read more here.
Keywords: cholinesterase inhibitory; inhibitory potency; affinity; directed ligands ... See more keywords
Multicomponent reactions as a privileged tool for multitarget-directed ligand strategies in Alzheimer's disease therapy.
Sign Up to like & getrecommendations! Published in 2022 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2022-0170
Abstract: Among neurodegenerative pathologies affecting the older population, Alzheimer's disease is the most common type of dementia and leads to neurocognitive and behavioral disorders. It is a complex and progressive age-related multifactorial disease characterized by a… read more here.
Keywords: multicomponent reactions; disease; alzheimer disease; directed ligand ... See more keywords