A novel class of benzamide-hydroxypyridinone (HPO) derivatives were innovatively designed, synthesised, and biologically evaluated as potential multitargeting candidates for the treatment of Alzheimer's disease (AD) through pharmacophores-merged approaches based on lead compounds 18d, benzyloxy phenyl analogs, and deferiprone (DFP). These hybrids possessed potent Monoamine oxidase B (MAO-B) inhibition as well as excellent iron chelation, with pFe3+ values ranging from 18.13 to 19.39. Among all the compounds, 8g exhibited the most potent selective MAO-B inhibitor (IC50 = 68.4 nM, SI = 213). Moreover, 8g showed favourable pharmacokinetic properties and had great potential to penetrate the BBB in silico and PAMPA-BBB assay. Molecular modelling...
International audienceIn the brains of patients with Alzheimer's disease, the enzymatic activities o...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...
Based on a multitarget strategy, a series of novel chromanone-1-benzyl-1,2,3,6-tetrahydropyridin hyb...
Based on a multitarget strategy, a series of novel chromanone–1-benzyl-1,2,3,6-tetrahydropyridin hyb...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
We discovered a small series of hit compounds that show multitargeting activities against key target...
Multifunctional agents aiming at cholinesterases (ChEs) and monoamine oxidases (MAOs) are promising ...
4th International Electronic Conference on Medicinal Chemistry (ECMC), ELECTR NETWORK, NOV 01-30, 20...
The design of multifunctional, neuroprotective compounds has received increasing attention due to th...
Monoamine oxidases (MAOs) are mitochondrial FAD-containing enzymes that catalyze the oxidative deami...
Alzheimer’s disease (AD) is a severe multifactorial neurodegenerative disorder characterized by a pr...
International audienceIn the brains of patients with Alzheimer's disease, the enzymatic activities o...
International audienceIn the brains of patients with Alzheimer's disease, the enzymatic activities o...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...
Based on a multitarget strategy, a series of novel chromanone-1-benzyl-1,2,3,6-tetrahydropyridin hyb...
Based on a multitarget strategy, a series of novel chromanone–1-benzyl-1,2,3,6-tetrahydropyridin hyb...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
The need for developing real disease-modifying drugs against neurodegenerative syndromes, particular...
We discovered a small series of hit compounds that show multitargeting activities against key target...
Multifunctional agents aiming at cholinesterases (ChEs) and monoamine oxidases (MAOs) are promising ...
4th International Electronic Conference on Medicinal Chemistry (ECMC), ELECTR NETWORK, NOV 01-30, 20...
The design of multifunctional, neuroprotective compounds has received increasing attention due to th...
Monoamine oxidases (MAOs) are mitochondrial FAD-containing enzymes that catalyze the oxidative deami...
Alzheimer’s disease (AD) is a severe multifactorial neurodegenerative disorder characterized by a pr...
International audienceIn the brains of patients with Alzheimer's disease, the enzymatic activities o...
International audienceIn the brains of patients with Alzheimer's disease, the enzymatic activities o...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...
Despite huge efforts to develop effective disease-modifying drug for Alzheimer disease (AD),the curr...