Search Results - "Stavrakov, Georgi"
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Ex Vivo Antioxidant and Cholinesterase Inhibiting Effects of a Novel Galantamine-Curcumin Hybrid on Scopolamine-Induced Neurotoxicity in Mice
Published in International journal of molecular sciences (27-11-2022)“…Oxidative stress is an essential factor in the development and progression of Alzheimer's disease (AD). An excessive amount of reactive oxygen species (ROS)…”
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2
A Novel Galantamine-Curcumin Hybrid as a Potential Multi-Target Agent against Neurodegenerative Disorders
Published in Molecules (Basel, Switzerland) (25-03-2021)“…The acetylcholinesterase (AChE) inhibitors are the main drugs for symptomatic treatment of neurodegenerative disorders like Alzheimer's disease. A recently…”
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3
A Galantamine-Curcumin Hybrid Decreases the Cytotoxicity of Amyloid-Beta Peptide on SH-SY5Y Cells
Published in International journal of molecular sciences (15-07-2021)“…Misfolded amyloid beta (Aβ) peptides aggregate and form neurotoxic oligomers. Membrane and mitochondrial damages, calcium dysregulation, oxidative stress, and…”
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A galantamine–curcumin hybrid lacks the depressant side effect of acetylcholinesterase inhibitors
Published in Biotechnology, biotechnological equipment (16-01-2024)“…AbstractAcetylcholinesterase inhibitors (AChEIs) are drugs that enhance cholinergic neuro-transmission and are used for the treatment of Alzheimer’s disease…”
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Discovery of a Novel Acetylcholinesterase Inhibitor by Fragment-Based Design and Virtual Screening
Published in Molecules (Basel, Switzerland) (03-04-2021)“…Despite extensive and intensive research efforts in recent decades, there is still no effective treatment for neurodegenerative diseases. On this background,…”
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Galantamine-Curcumin Hybrids as Dual-Site Binding Acetylcholinesterase Inhibitors
Published in Molecules (Basel, Switzerland) (23-07-2020)“…Galantamine (GAL) and curcumin (CU) are alkaloids used to improve symptomatically neurodegenerative conditions like Alzheimer's disease (AD). GAL acts mainly…”
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Novel hits for acetylcholinesterase inhibition derived by docking-based screening on ZINC database
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2018)“…The inhibition of the enzyme acetylcholinesterase (AChE) increases the levels of the neurotransmitter acetylcholine and symptomatically improves the affected…”
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8
Camphane-based aminophosphine ligands for Pd-catalyzed asymmetric allylic alkylation
Published in Tetrahedron: asymmetry (31-10-2013)“…A practical synthesis of new chiral aminophosphine ligands based on the camphane scaffold bearing alkoxy groups was accomplished. The application of these…”
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From Central to Axial to Central Chirality: Enantioselective Construction of the trans-4,5,9,10-Tetrahydroxy-9,10-dihydrophenanthrene System
Published in European Journal of Organic Chemistry (01-12-2007)“…Enantioselective synthesis of the core trans‐4,5,9,10‐tetrahydroxy‐9,10‐dihydrophenanthrene parent system of the antibiotics benanimicin, pradimicin and FD 594…”
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AChE inhibitory activity of N-substituted natural galanthamine derivatives
Published in Bioorganic & medicinal chemistry letters (01-11-2024)“…[Display omitted] •Complete NMR data of N-acethylnorgalanthamine has been provided.•The N-substituent of galanthamine derivatives influences the binding…”
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Galantamine derivatives: Synthesis, NMR study, DFT calculations and application in asymmetric catalysis
Published in Journal of molecular structure (05-11-2020)“…In a search of effective ligands for asymmetric catalysis (−)-galantamine has been selected as a complex chiral framework for the synthesis of four novel…”
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Galantamine derivatives with indole moiety: Docking, design, synthesis and acetylcholinesterase inhibitory activity
Published in Bioorganic & medicinal chemistry (01-09-2015)“…[Display omitted] The inhibitors of acetylcholinesterase are the main therapy against Alzheimer’s disease. Among them, galantamine is the best tolerated and…”
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13
Ferrocene modified analogues of imatinib and nilotinib as potent anti-cancer agents
Published in RSC medicinal chemistry (25-05-2023)“…The unique features of ferrocene and the need for development of targeted anticancer drugs inspired the design, synthesis and biological evaluation of…”
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14
Theophylline-7-acetic acid derivatives with amino acids as anti-tuberculosis agents
Published in Bioorganic & medicinal chemistry letters (15-07-2014)“…A series of amides were synthesized by condensation of theophylline-7-acetic acid and eight commercially available amino acid methyl ester hydrochlorides…”
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15
Novel camphane-based anti-tuberculosis agents with nanomolar activity
Published in European journal of medicinal chemistry (01-12-2013)“…A series of new amidoalcohols and amidodiols were designed on the base of the camphor scaffold and evaluated for their in vitro activity against Mycobacterium…”
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Synthetic piperine amide analogs with antimycobacterial activity
Published in Chemical biology & drug design (01-03-2018)“…Piperine amide analogs are synthesized by replacement of the piperidine moiety with different types of cyclic amines, including adamantyl and…”
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Synthesis and antimycobacterial activity of novel camphane-based agents
Published in Bioorganic & medicinal chemistry letters (01-01-2014)“…A series of six new amidoalcohols was designed and synthesized on the base of the camphor scaffold. Natural amino acids were transformed into their α-hydroxy…”
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Docking‐based design and synthesis of galantamine–camphane hybrids as inhibitors of acetylcholinesterase
Published in Chemical biology & drug design (01-11-2017)“…Galantamine (GAL) as an acetylcholinesterase inhibitor (AChEI) is among the main drugs approved for the treatment of Alzheimer's disease. It fits perfectly…”
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19
Docking-based Design of Galantamine Derivatives with Dual-site Binding to Acetylcholinesterase
Published in Molecular informatics (01-07-2016)“…The enzyme acetylcholinesterase is a key target in the treatment of Alzheimer's disease because of its ability to hydrolyze acetylcholine via the catalytic…”
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Camphane-based phosphino-carboxamide ligands as P,O-chelates in Pd-catalyzed enantioselective allylic alkylation
Published in Tetrahedron: asymmetry (15-07-2012)“…A practical synthesis for new chiral phosphino-carboxamide ligands has been accomplished. These ligands were effectively modified both on the amide moiety and…”
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