Synthesis and biological evaluation of Halogen-Substituted novel α-Ketoamides as potential protein aggregation modulators in Alzheimer's disease
In this study, a series of α-ketoamide derivatives was synthesized from β,γ-unsaturated α-keto thioesters, achieving high purity and good yield. Thioflavin T based Aβ aggregation assay identified four promising compounds (BD19, BD23, BD24, and BD27) that demonstrated significant inhibitory effects on Aβ aggregation. BD23, selected for its better solubility (0.045 ± 0.0012 mg/ml), was further subjected to in vitro Parallel Artificial Membrane Permeability Assay to determine the Blood-Brain-Barrier permeability and emerged as BBB permeable with permeability rate (Pe) of 10.66 ± 8.11 × 10-6 cm/s. In addition to its A...
Source: Bioorganic Chemistry - April 23, 2024 Category: Chemistry Authors: Bhanuranjan Das Anurag Tk Baidya Sourabh Chakrabarti Deepak Chouhan Banita Thakur Taher Darreh-Shori Gefei Chen Vinod Tiwari Rajnish Kumar Source Type: research
Synthesis and biological evaluation of Halogen-Substituted novel α-Ketoamides as potential protein aggregation modulators in Alzheimer's disease
In this study, a series of α-ketoamide derivatives was synthesized from β,γ-unsaturated α-keto thioesters, achieving high purity and good yield. Thioflavin T based Aβ aggregation assay identified four promising compounds (BD19, BD23, BD24, and BD27) that demonstrated significant inhibitory effects on Aβ aggregation. BD23, selected for its better solubility (0.045 ± 0.0012 mg/ml), was further subjected to in vitro Parallel Artificial Membrane Permeability Assay to determine the Blood-Brain-Barrier permeability and emerged as BBB permeable with permeability rate (Pe) of 10.66 ± 8.11 × 10-6 cm/s. In addition to its A...
Source: Bioorganic Chemistry - April 23, 2024 Category: Chemistry Authors: Bhanuranjan Das Anurag Tk Baidya Sourabh Chakrabarti Deepak Chouhan Banita Thakur Taher Darreh-Shori Gefei Chen Vinod Tiwari Rajnish Kumar Source Type: research
Predicting the efficacy of donepezil intervention in Alzheimer's disease patients using regional homogeneity in the inferior orbitofrontal cortex
CONCLUSIONS: These findings deepen our understanding of the brain mechanisms underlying the clinical efficacy of donepezil in AD patients, and provide a novel way to predict its clinical efficacy in such patients.PMID:38630202 | DOI:10.1007/s40520-023-02691-6 (Source: Aging Clinical and Experimental Research)
Source: Aging Clinical and Experimental Research - April 17, 2024 Category: Geriatrics Authors: Min Dai Zhongwei Guo Honglian Xia Hong Zhu Jiapeng Li Hongtao Hou Guizhi Zhao Xiaozheng Liu Source Type: research
Predicting the efficacy of donepezil intervention in Alzheimer's disease patients using regional homogeneity in the inferior orbitofrontal cortex
CONCLUSIONS: These findings deepen our understanding of the brain mechanisms underlying the clinical efficacy of donepezil in AD patients, and provide a novel way to predict its clinical efficacy in such patients.PMID:38630202 | PMC:PMC11024046 | DOI:10.1007/s40520-023-02691-6 (Source: Aging Clinical and Experimental Research)
Source: Aging Clinical and Experimental Research - April 17, 2024 Category: Geriatrics Authors: Min Dai Zhongwei Guo Honglian Xia Hong Zhu Jiapeng Li Hongtao Hou Guizhi Zhao Xiaozheng Liu Source Type: research
Ameliorative anti-coagulant, anti-oxidative and anti-ferroptotic activities of nanocurcumin and donepezil on coagulation, oxidation and ferroptosis in Alzheimer's disease
The objective of the current investigation was to examine the neuroprotective and anti-ferroptotic role of nanocurcumin and Donepezil against model of aluminum chloride AlCl3 and D-galactose induced ad. The experiment was performed on 70 rats divided into (G1: control, G2: NCMN, G3: Donepezil, G4: ad-model, G5: Donepezil co-treatment, G6: NCMN co-treatment and G7: NCMN+Donepezil co-treatment). Hematological parameters and biochemical investigations as oxidative stress, liver function, kidney function, iron profile and plasma fibrinogen were evaluated. Treatment with Nanocurcumin alone or in combination with Donepezil impro...
Source: Cell Research - April 15, 2024 Category: Cytology Authors: Nagat F Nawar Doha M Beltagy Tarek M Mohamed Ehab Tousson Mai M El-Keey Source Type: research
Review on anti-alzheimer drug development: approaches, challenges and perspectives
RSC Adv. 2024 Apr 5;14(16):11057-11088. doi: 10.1039/d3ra08333k. eCollection 2024 Apr 3.ABSTRACTAlzheimer is an irreversible progressive neurodegenerative disease that causes failure of cerebral neurons and disability of the affected person to practice normal daily life activities. There is no concrete evidence to identify the exact reason behind the disease, so several relevant hypotheses emerged, highlighting many possible therapeutic targets, such as acetylcholinesterase, cholinergic receptors, N-methyl d-aspartate receptors, phosphodiesterase, amyloid β protein, protein phosphatase 2A, glycogen synthase kinase-3 beta,...
Source: Adv Data - April 8, 2024 Category: Epidemiology Authors: Abdallah E Abdallah Source Type: research
Review on anti-alzheimer drug development: approaches, challenges and perspectives
RSC Adv. 2024 Apr 5;14(16):11057-11088. doi: 10.1039/d3ra08333k. eCollection 2024 Apr 3.ABSTRACTAlzheimer is an irreversible progressive neurodegenerative disease that causes failure of cerebral neurons and disability of the affected person to practice normal daily life activities. There is no concrete evidence to identify the exact reason behind the disease, so several relevant hypotheses emerged, highlighting many possible therapeutic targets, such as acetylcholinesterase, cholinergic receptors, N-methyl d-aspartate receptors, phosphodiesterase, amyloid β protein, protein phosphatase 2A, glycogen synthase kinase-3 beta,...
Source: Adv Data - April 8, 2024 Category: Epidemiology Authors: Abdallah E Abdallah Source Type: research
Potential acetylcholinesterase inhibitors to treat Alzheimer's disease
CONCLUSIONS: This study found that Z-9 (Fluoroquinolones) and TBAF-6 (benzimidazole-benzothiazole) compounds improve behavioral and biochemical parameters, thus treating neurodegenerative disorders effectively.PMID:38567612 | DOI:10.26355/eurrev_202403_35759 (Source: Pharmacological Reviews)
Source: Pharmacological Reviews - April 3, 2024 Category: Drugs & Pharmacology Authors: A Saud V Krishnaraju A Taha K Kalpana V Malarkodi S Durgaramani V Vinoth Prabhu F A Saleh S Ezhilarasan Source Type: research
Aurothioglucose encapsulated nanoparticles fostered neuroprotection in streptozotocin-induced Alzheimer's disease
This study was planned to prepare the PLGA nanoparticles of aurothioglucose (ATG) and check the neuroprotective potential against STZ-induced AD in rats. The nanoparticles were prepared using the double emulsion solvent evaporation method and characterized for various parameters such as drug-excipient interaction, particle size, zeta potential, and morphology. Then, rats were injected STZ (3 mg/kg/i.c.v., days 1 and 3) and ATG (5 and 10 mg/kg/s.c.), ATG NPs (2.5 and 5 mg/kg/s.c.) and donepezil (2 mg/kg/p.o) from 15th to 29th day. Behavior parameters were performed using an actophotometer, MWM, and ORT. On the 30th day, all...
Source: Brain Research - April 3, 2024 Category: Neurology Authors: Shiv Kumar Kushawaha Mahendra Singh Ashawat Divya Soni Puneet Kumar None Rimpi Ashish Baldi Source Type: research
Potential acetylcholinesterase inhibitors to treat Alzheimer's disease
CONCLUSIONS: This study found that Z-9 (Fluoroquinolones) and TBAF-6 (benzimidazole-benzothiazole) compounds improve behavioral and biochemical parameters, thus treating neurodegenerative disorders effectively.PMID:38567612 | DOI:10.26355/eurrev_202403_35759 (Source: European Review for Medical and Pharmacological Sciences)
Source: European Review for Medical and Pharmacological Sciences - April 3, 2024 Category: Drugs & Pharmacology Authors: A Saud V Krishnaraju A Taha K Kalpana V Malarkodi S Durgaramani V Vinoth Prabhu F A Saleh S Ezhilarasan Source Type: research
Potential acetylcholinesterase inhibitors to treat Alzheimer's disease
CONCLUSIONS: This study found that Z-9 (Fluoroquinolones) and TBAF-6 (benzimidazole-benzothiazole) compounds improve behavioral and biochemical parameters, thus treating neurodegenerative disorders effectively.PMID:38567612 | DOI:10.26355/eurrev_202403_35759 (Source: Pharmacological Reviews)
Source: Pharmacological Reviews - April 3, 2024 Category: Drugs & Pharmacology Authors: A Saud V Krishnaraju A Taha K Kalpana V Malarkodi S Durgaramani V Vinoth Prabhu F A Saleh S Ezhilarasan Source Type: research
Aurothioglucose encapsulated nanoparticles fostered neuroprotection in streptozotocin-induced Alzheimer's disease
This study was planned to prepare the PLGA nanoparticles of aurothioglucose (ATG) and check the neuroprotective potential against STZ-induced AD in rats. The nanoparticles were prepared using the double emulsion solvent evaporation method and characterized for various parameters such as drug-excipient interaction, particle size, zeta potential, and morphology. Then, rats were injected STZ (3 mg/kg/i.c.v., days 1 and 3) and ATG (5 and 10 mg/kg/s.c.), ATG NPs (2.5 and 5 mg/kg/s.c.) and donepezil (2 mg/kg/p.o) from 15th to 29th day. Behavior parameters were performed using an actophotometer, MWM, and ORT. On the 30th day, all...
Source: Brain Research - April 3, 2024 Category: Neurology Authors: Shiv Kumar Kushawaha Mahendra Singh Ashawat Divya Soni Puneet Kumar None Rimpi Ashish Baldi Source Type: research
Potential acetylcholinesterase inhibitors to treat Alzheimer's disease
CONCLUSIONS: This study found that Z-9 (Fluoroquinolones) and TBAF-6 (benzimidazole-benzothiazole) compounds improve behavioral and biochemical parameters, thus treating neurodegenerative disorders effectively.PMID:38567612 | DOI:10.26355/eurrev_202403_35759 (Source: European Review for Medical and Pharmacological Sciences)
Source: European Review for Medical and Pharmacological Sciences - April 3, 2024 Category: Drugs & Pharmacology Authors: A Saud V Krishnaraju A Taha K Kalpana V Malarkodi S Durgaramani V Vinoth Prabhu F A Saleh S Ezhilarasan Source Type: research
