piroxicam and coumarin

piroxicam has been researched along with coumarin* in 4 studies

Other Studies

4 other study(ies) available for piroxicam and coumarin

ArticleYear
Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2018, Feb-25, Volume: 146

    Topics: Acetylcholinesterase; Alzheimer Disease; Amyloid beta-Peptides; Animals; Blood-Brain Barrier; Cell Line, Tumor; Cholinesterase Inhibitors; Coumarins; Dose-Response Relationship, Drug; Drug Design; Humans; Kinetics; Male; Mice; Mice, Inbred Strains; Models, Molecular; Molecular Structure; Peptide Fragments; Protein Aggregates; Range of Motion, Articular; Structure-Activity Relationship; Thiocarbamates

2018
Design, synthesis and evaluation of coumarin-pargyline hybrids as novel dual inhibitors of monoamine oxidases and amyloid-β aggregation for the treatment of Alzheimer's disease.
    European journal of medicinal chemistry, 2017, Sep-29, Volume: 138

    A series of coumarin-pargyline hybrids (4a-x) have been designed, synthesized and evaluated as novel dual inhibitors of Alzheimer's disease (AD). Most of the compounds exhibited a potent ability to inhibit amyloid-β (Aβ) aggregation and monoamine oxidases. In particular, compound 4x exhibited remarkable inhibitory activities against monoamine oxidases (IC

    Topics: Alzheimer Disease; Amyloid beta-Peptides; Animals; Cell Survival; Coumarins; Dose-Response Relationship, Drug; Drug Design; Humans; Male; Mice; Mice, Inbred Strains; Molecular Structure; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Pargyline; PC12 Cells; Protein Aggregates; Rats; Structure-Activity Relationship

2017
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
    Bioorganic & medicinal chemistry, 2016, Apr-01, Volume: 24, Issue:7

    Combining N-benzylpiperidine moiety of donepezil and coumarin into in a single molecule, novel hybrids with ChE and MAO-B inhibitory activity were designed and synthesized. The biological screening results indicated that most of compounds displayed potent inhibitory activity for AChE and BuChE, and clearly selective inhibition to MAO-B. Of these compounds, 5m was the most potent inhibitor for eeAChE and eqBuChE (0.87 μM and 0.93 μM, respectively), and it was also a good and balanced inhibitor to hChEs and hMAO-B (1.37 μM for hAChE; 1.98 μM for hBuChE; 2.62 μM for hMAO-B). Molecular modeling and kinetic studies revealed that 5m was a mixed-type inhibitor, which bond simultaneously to CAS, PAS and mid-gorge site of AChE, and it was also a competitive inhibitor, which occupied the active site of MAO-B. In addition, 5m showed good ability to cross the BBB and had no toxicity on SH-SY5Y neuroblastoma cells. Collectively, all these results suggested that 5m might be a promising multi-target lead candidate worthy of further pursuit.

    Topics: Alzheimer Disease; Animals; Butyrylcholinesterase; Cell Line, Tumor; Cholinesterase Inhibitors; Cholinesterases; Coumarins; Donepezil; Dose-Response Relationship, Drug; Drug Design; Eels; Humans; Indans; Models, Molecular; Molecular Structure; Molecular Targeted Therapy; Piperidines; Structure-Activity Relationship

2016
Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
    European journal of medicinal chemistry, 2015, May-05, Volume: 95

    A series of novel tacrine-coumarin hybrids were designed, synthesized and evaluated as multi-target agents against Alzheimer's disease. The biological assays indicated that most of compounds displayed potent inhibitory activity toward AChE and BuChE, and clearly selective inhibition for MAO-B. Among these compounds, 14c exhibited strong inhibitory activity for AChE (IC50 values of 33.63 nM for eeAChE and 16.11 nM for hAChE) and BuChE (IC50 values of 80.72 nM for eqBuChE and 112.72 nM for hBuChE), and the highest inhibitory activity against hMAO-B (IC50 value of 0.24 μM). Kinetic and molecular modeling studies revealed that 14c was a mixed-type inhibitor, binding simultaneously to catalytic, peripheral and mid-gorge sites of AChE. It was also a competitive inhibitor, which covered the substrate and entrance cavities of MAO-B. Moreover, 14c could penetrate the CNS and show low cell toxicity. Overall, these results suggested that 14c might be an excellent multi-target agent for AD treatment.

    Topics: Acetylcholinesterase; Alzheimer Disease; Benzopyrans; Blood-Brain Barrier; Brain; Cell Survival; Cells, Cultured; Cholinesterase Inhibitors; Coumarins; Drug Design; Erythrocytes; Humans; Kinetics; Models, Molecular; Molecular Docking Simulation; Monoamine Oxidase; Monoamine Oxidase Inhibitors; Neuroblastoma; Piperazines; Tacrine

2015