Design, synthesis, and structure–activity relationship of caffeine‐based triazoles as dual AChE and BACE‐1 inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.21998
Abstract: Natural products have significantly contributed to drug discovery for neurodegenerative diseases. Caffeine is one of the well‐known central nervous system(CNS)‐active natural products. Besides its CNS stimulant properties, it is a mild inhibitor of acetylcholinesterase (AChE)… read more here.
Keywords: bace; caffeine based; caffeine; ache ... See more keywords
Multitargeted C9‐substituted ester and ether derivatives of berberrubine for Alzheimer's disease: Design, synthesis, biological evaluation, metabolic stability, and pharmacokinetics
Sign Up to like & getrecommendations! Published in 2022 at "Drug Development Research"
DOI: 10.1002/ddr.22017
Abstract: Berberrubine is a naturally occurring isoquinoline alkaloid and a bioactive metabolite of berberine. Berberine exhibits a wide range of pharmacological activities, including cholinesterase inhibition. The cholinesterase inhibitors provide symptomatic treatment for Alzheimer's disease; however, multitarget‐directed… read more here.
Keywords: bace; inhibition; ester; disease ... See more keywords
Synthesis of new N‐(5,6‐methylenedioxybenzothiazole‐2‐yl)‐2‐[(substituted)thio/piperazine]acetamide/propanamide derivatives and evaluation of their AChE, BChE, and BACE‐1 inhibitory activities
Sign Up to like & getrecommendations! Published in 2024 at "Drug Development Research"
DOI: 10.1002/ddr.22214
Abstract: In this study, the synthesis of N‐(5,6‐methylenedioxybenzothiazole‐2‐yl)‐2‐[(substituted)thio/piperazine]acetamide/propanamide derivatives (3a‐3k) and to investigate their acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and β‐secretase 1 (BACE‐1) inhibition activity were aimed. Mass, 1H NMR, and 13C NMR spectra were utilized to… read more here.
Keywords: bche; methylenedioxybenzothiazole substituted; bace; substituted thio ... See more keywords
Effect of sampling on BACE‐1 ligands binding free energy predictions via MM‐PBSA calculations
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Computational Chemistry"
DOI: 10.1002/jcc.24839
Abstract: The BACE‐1 enzyme is a prime target to find a cure to Alzheimer's disease. In this article, we used the MM‐PBSA approach to compute the binding free energies of 46 reported ligands to this enzyme.… read more here.
Keywords: bace; effect sampling; bace ligands; sampling bace ... See more keywords
Identification of Cannabidiolic and Cannabigerolic Acids as MTDL AChE, BuChE, and BACE‐1 Inhibitors Against Alzheimer's Disease by In Silico, In Vitro, and In Vivo Studies
Sign Up to like & getrecommendations! Published in 2024 at "Phytotherapy Research"
DOI: 10.1002/ptr.8369
Abstract: Cannabidiolic (CBDA) and cannabigerolic (CBGA) acids are naturally occurring compounds from Cannabis sativa plant, previously identified by us as dual PPARα/γ agonists. Since the development of multitarget‐directed ligands (MTDL) represents a valuable strategy to alleviate… read more here.
Keywords: cbga; ache buche; bace; cbda cbga ... See more keywords
The potential of natural product vs neurodegenerative disorders: In silico study of artoflavanocoumarin as BACE-1 inhibitor
Sign Up to like & getrecommendations! Published in 2018 at "Computational biology and chemistry"
DOI: 10.1016/j.compbiolchem.2018.10.015
Abstract: Increasing evidence suggests the beneficial impact of flavonoid-rich nutrition on normal cognitive function. It has been revealed that flavonoids can slow neurodegenerative processes in situations such as Alzheimer's disease (AD). The β-secretase (BACE-1) is one… read more here.
Keywords: bace; silico study; study; study artoflavanocoumarin ... See more keywords
Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.07.006
Abstract: In this paper, the preparation of a new class of multi-target-directed ligands (MTDLs) based on a 7-amino-1,4-dihydro-2H-isoquilin-3-one, whose lead (compound I) showed promising properties in acetylcholinesterase (AChE) inhibitory activity [1], is described. The results of… read more here.
Keywords: bace; ache; isoquilin one; amino dihydro ... See more keywords
BACE inhibitor treatment of mice induces hyperactivity in a Seizure-related gene 6 family dependent manner without altering learning and memory
Sign Up to like & getrecommendations! Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-94369-0
Abstract: BACE inhibitors, which decrease BACE1 (β-secretase 1) cleavage of the amyloid precursor protein, are a potential treatment for Alzheimer’s disease. Clinical trials using BACE inhibitors have reported a lack of positive effect on patient symptoms… read more here.
Keywords: bace; treatment; family; mice ... See more keywords
BACE inhibitors in clinical development for the treatment of Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2018 at "Expert Review of Neurotherapeutics"
DOI: 10.1080/14737175.2018.1531706
Abstract: ABSTRACT Introduction: The amyloid hypothesis of Alzheimer’s disease (AD) affirms that brain accumulation of amyloid-β (Aβ) oligomers and soluble aggregates represent the major pathological event of the disease. Several anti-Aβ small organic molecules, monoclonal antibodies… read more here.
Keywords: bace; alzheimer disease; treatment; bace inhibitors ... See more keywords
Targeted BACE-1 inhibition in microglia enhances amyloid clearance and improved cognitive performance
Sign Up to like & getrecommendations! Published in 2022 at "Science Advances"
DOI: 10.1126/sciadv.abo3610
Abstract: Abnormal accumulation of β-amyloid (Aβ) peptides is a culprit in Alzheimer’s disease (AD); blocking Aβ generation is therefore being explored as a logical approach for AD treatment. Here, we demonstrate that targeted inhibition of β-site… read more here.
Keywords: clearance; bace; inhibition; bace microglia ... See more keywords
Efficacy and safety of bronchial arterial chemoembolization (BACE) in combination with tislelizumab for non-small cell lung cancer (NSCLC): A phase II study.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2024.42.16_suppl.8609
Abstract: 8609 Background: Bronchial artery chemoembolization (BACE) and immune checkpoint inhibitors (ICIs) are important therapy for NSCLC. The short-term benefit from BACE is considerable while the long-term survival benefits from ICIs is remarkable. This trial is… read more here.
Keywords: chemoembolization bace; bace; safety; study ... See more keywords