Sulfonamide derivatives as multi-target agents for complex diseases
Sulfonamide derivatives are frequently seen structural motifs in medicinal chemistry. Almost
a century after Gerhard Domagk's pioneering work leading to the first sulfonamide antibiotic …
a century after Gerhard Domagk's pioneering work leading to the first sulfonamide antibiotic …
Comparison of the binding of reversible inhibitors to human butyrylcholinesterase and acetylcholinesterase: A crystallographic, kinetic and calorimetric study
TL Rosenberry, X Brazzolotto, IR Macdonald… - Molecules, 2017 - mdpi.com
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) hydrolyze the
neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic …
neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic …
Mitochondria as a promising target for developing novel agents for treating Alzheimer's disease
EF Shevtsova, AV Maltsev… - Medicinal Research …, 2021 - Wiley Online Library
The mitochondria‐targeting drugs can be conventionally divided into the following groups:
those compensating for the energy deficit involved in neurodegeneration, including …
those compensating for the energy deficit involved in neurodegeneration, including …
The magic of crystal structure-based inhibitor optimization: development of a butyrylcholinesterase inhibitor with picomolar affinity and in vivo activity
U Kosak, B Brus, D Knez, S Zakelj… - Journal of medicinal …, 2018 - ACS Publications
The enzymatic activity of butyrylcholinesterase (BChE) in the brain increases with the
progression of Alzheimer's disease, thus classifying BChE as a promising drug target in …
progression of Alzheimer's disease, thus classifying BChE as a promising drug target in …
Design, Synthesis, and Proof of Concept of Balanced Dual Inhibitors of Butyrylcholinesterase (BChE) and Histone Deacetylase 6 (HDAC6) for the Treatment of …
L Wang, T Sun, Z Wang, H Liu, W Qiu… - ACS chemical …, 2023 - ACS Publications
Concomitant inhibition of butyrylcholinesterase (BChE) and histone deacetylase 6 (HDAC6)
is supposed to be effective in the treatment of Alzheimer's disease (AD). Inspired by our …
is supposed to be effective in the treatment of Alzheimer's disease (AD). Inspired by our …
Photoswitchable Pseudoirreversible Butyrylcholinesterase Inhibitors Allow Optical Control of Inhibition in Vitro and Enable Restoration of Cognition in an Alzheimer's …
M Scheiner, A Sink, M Hoffmann… - Journal of the …, 2022 - ACS Publications
To develop tools to investigate the biological functions of butyrylcholinesterase (BChE) and
the mechanisms by which BChE affects Alzheimer's disease (AD), we synthesized several …
the mechanisms by which BChE affects Alzheimer's disease (AD), we synthesized several …
N-Benzyl Benzamide Derivatives as Selective Sub-Nanomolar Butyrylcholinesterase Inhibitors for Possible Treatment in Advanced Alzheimer's Disease
C Du, L Wang, Q Guan, H Yang, T Chen… - Journal of Medicinal …, 2022 - ACS Publications
Herein, we report a series of selective sub-nanomolar inhibitors against
butyrylcholinesterase (BChE). These compounds, bearing a novel N-benzyl benzamide …
butyrylcholinesterase (BChE). These compounds, bearing a novel N-benzyl benzamide …
Selective pseudo-irreversible butyrylcholinesterase inhibitors transferring antioxidant moieties to the enzyme show pronounced neuroprotective efficacy in vitro and in …
M Scheiner, M Hoffmann, F He, E Poeta… - Journal of Medicinal …, 2021 - ACS Publications
A series of multitarget-directed ligands (MTDLs) was designed by functionalizing a pseudo-
irreversible butyrylcholinesterase (BChE) inhibitor. The obtained hybrids were investigated …
irreversible butyrylcholinesterase (BChE) inhibitor. The obtained hybrids were investigated …
Inhibition of acetylcholinesterase and butyrylcholinesterase with uracil derivatives: kinetic and computational studies
Abstract Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) inhibitors are
interesting compounds for different therapeutic applications, among which Alzheimer's …
interesting compounds for different therapeutic applications, among which Alzheimer's …
Tryptophan-derived butyrylcholinesterase inhibitors as promising leads against Alzheimer's disease
We have identified tryptophan-based selective nanomolar butyrylcholinesterase (BChE)
inhibitors. They are defined according to their chemical modularity, novel binding mode …
inhibitors. They are defined according to their chemical modularity, novel binding mode …