Discovery of a Potent and Selective MAO‐B Inhibitor From a Donepezil‐Linked Chalcone Library With Promising Antiparkinsonian Activity [PDF]
ABSTRACT A focused library of 19 donepezil‐linked chalcones (DLCs) was efficiently synthesised through microwave‐assisted Claisen‐Schmidt condensation and subsequently profiled for their inhibitory activities against cholinesterases (AChE and BuChE) as well as monoamine oxidases (MAO‐A and MAO‐B).
Azize Kirac‐Aydin +11 more
wiley +2 more sources
Monoamine Oxidase and Cholinesterase Inhibition Profiles of Semicarbazone and Thiosemicarbazone Derivatives [PDF]
Thiosemicarbazones generally show higher MAO‐B inhibitory potential than their corresponding semicarbazones, and particularly T6 is the most potent, which contains R = H and X = S in its Tail Unit, with an IC50 value of 6.45 µM with SI of 3.6. ABSTRACT Twenty semicarbazone and thiosemicarbazone derivatives (T1–T20) were synthesized and evaluated for ...
Sandeep Bindra +11 more
wiley +2 more sources
From Fragments to Function: Novel Hydrazone Derivatives as Monoamine Oxidase Inhibitors [PDF]
Twelve N‐acylhydrazone derivatives (5a–f, 6a–f) were synthesized and characterized. Compounds displayed potent submicromolar inhibition against both MAO‐A and MAO‐B. Compound 6e exhibited the strongest activity (IC50 = 0.073 μM for MAO‐A; 0.064 μM for MAO‐B). Kinetic and docking analyses confirmed reversible, competitive inhibition via FAD interaction.
Hasan Erdinç Sellitepe +5 more
wiley +2 more sources
AbstractPyridoxamine inhibits rabbit and pig plasma benzylamine oxidase (BAO), the diamine oxidase of pig kidney and the lysyloxidase of pig aorta in-vitro. In-vivo in the rabbit, the inhibitory activity of pyridoxamine on plasma BAO is antagonized by an increase in the level of this enzyme that is dependent on an increase in rate of synthesis, there ...
BUFFONI, FRANCA +6 more
core +6 more sources
Exploring Disulfide Bridge as a Tool to Improve Pioglitazone’s Neuroprotective Potential: Toward the Development of Prolonged‐Acting MAO‐B/PPARγ Modulators [PDF]
Pioglitazone is an antidiabetic drug acting as a peroxisome proliferator‐activated receptor γ (PPARγ) agonist and later repositioned as a monoamine oxidase B (MAO‐B) inhibitor. Despite promising preclinical premises, it showed a lack of efficacy in clinical trials as a treatment for neurodegenerative diseases.
Filippo Basagni +12 more
wiley +2 more sources
A Renal Clearable Probe for In Vivo Monoamine Oxidase (MAO) Detection [PDF]
A renal‐clearable Cy7‐based fluorogenic probe enables rapid and non‐invasive detection of monoamine oxidase (MAO) activity in vivo. Upon MAO‐mediated activation, the fluorescent product is efficiently excreted in urine, allowing direct quantification of enzyme overexpression.
Marcia Domínguez +13 more
wiley +2 more sources
A Sulfonamide Intermediate Elicits Therapeutic Effect Against Sepsis by Enhancing Neutrophil Maturation [PDF]
ABSTRACT Sepsis, a life‐threatening condition characterized by systemic inflammation and immune dysregulation, remains a major cause of mortality worldwide. Here, we identify a synthetic sulfonamide intermediate, 1‐[5‐(2‐fluorophenyl)furan‐2‐yl]‐N‐(4‐methylbenzyl)methanamine (FMM), as a host‐directed therapeutic candidate that enhances neutrophil ...
Ji Ye Park +10 more
wiley +2 more sources
Age-related changes in benzylamine oxidase activity in rat tissues
AbstractBrain, liver, heart, lung, kidney and duodenum benzylamine oxidase (BZAO) activities were measured from young and old rats. Protein content was found to decrease in liver (-17%), kidney (-20%) and duodenum (-17%) but remained unchanged in brain, heart and lung of old rats compared with that of young rats.
H, Cao Danh +3 more
openaire +3 more sources
Nanomaterial Integration at Liquid–Liquid Interfaces for Green Catalysis [PDF]
Functional nanomaterials assembled at liquid–liquid interfaces create dual‐role platforms serving as emulsion stabilizers and catalytic sites, offering enhanced reaction kinetics with improved catalyst recovery and recyclability. This review examines design strategies, structure‐performance relationships, and industrial implementation prospects of ...
Bokgi Seo +6 more
wiley +2 more sources
Towards the directed evolution of an L-aspartate oxidase from Pseudomonas putida [PDF]
Amino acid oxidases (AAOs) are enantioselective flavoenzymes that catalyse the oxidation of amino acids into imino acids, which spontaneously hydrolyse in water to form keto acids. AAOs have several potential applications, most notably as biocatalysts in
Leese, Charlotte
core +6 more sources

