A5076428995- Chemical Synthesis and Analysis
- Chemistry and Chemical Engineering
- Biochemical and Structural Characterization
- Computational Drug Discovery Methods
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Chemical Synthesis and Reactions
- Cholinesterase and Neurodegenerative Diseases
- Catalytic Cross-Coupling Reactions
- Various Chemistry Research Topics
- Analytical Chemistry and Chromatography
- Asymmetric Synthesis and Catalysis
- Cyclopropane Reaction Mechanisms
- Analytical Methods in Pharmaceuticals
- Catalytic C–H Functionalization Methods
- Click Chemistry and Applications
- Nanomaterials for catalytic reactions
- Antibiotics Pharmacokinetics and Efficacy
- Innovative Microfluidic and Catalytic Techniques Innovation
- Alzheimer's disease research and treatments
- Medicinal Plants and Neuroprotection
- Peptidase Inhibition and Analysis
University of Bologna
2020-2023
Institute of Protein Biochemistry
2022
Alma Mater Europaea
2021
Developing greener synthesis processes is an inescapable necessity to transform the industrial landscape, mainly in pharmaceutical sector, into a long-term, sustainable reality.
A green protocol for SPPS allows the recovery and recycling of solvents bases from process waste mixture.
A fast and greensolution-phase peptide synthesis (GSolPPS) via continuous protocol, addressed with propylphosphonic anhydride T3P® as coupling reagent N -benzyloxycarbonyl-protecting group easily removed by hydrogenation is herein reported.
The identification of a green, versatile, user-friendly, and efficient methodology is necessary to facilitate the use Heck-Cassar-Sonogashira (HCS) cross-coupling reaction in drug discovery industrial production pharmaceutical segment. Heck-Cassar Sonogashira protocols, using N-hydroxyethylpyrrolidone (HEP)/water/N,N,N',N'-tetramethyl guanidine (TMG) as green solvent/base mixture sulfonated phosphine ligands, allowed recycle catalyst, always guaranteeing high yields fast conversion under...
Solid Phase Peptide Synthesis (SPPS) is a key technology for the production of pharmaceutical grade peptides and replacement piperidine with alternative bases piece puzzle moving toward greener technology.
Starting from six potential hits identified in a virtual screening campaign directed to cryptic pocket of BACE-1, at the edge catalytic cleft, we have synthesized and evaluated hybrid compounds, designed simultaneously reach BACE-1 secondary sites exert additional activities interest for Alzheimer's disease (AD). We lead compound with potent vitro activity towards human cholinesterases, moderate Aβ42 tau antiaggregating activity, brain permeability, which is nontoxic neuronal cells zebrafish...
The enantioselective 1,3-dipolar cycloaddition of nitrones and arylpropionaldehydes to generate highly functionalized scaffolds for application in drug discovery was herein investigated. use a second-generation MacMillan catalyst as hydrochloride salt consistently accelerated the reaction speed, allowing decrease time up >100 times, still affording 4-isoxazolines with good excellent enantiomeric ratios at room temperature. As proof concept, further functionalization isoxazoline core through...
The growing applications of peptide-based therapeutics require the development efficient protocols from perspective an industrial scale-up. T3P® (cyclic propylphosphonic anhydride) promotes amidation in solution-phase through a biomimetic approach, similar to activation carboxylic moiety catalyzed by ATP-grasp enzymes metabolic pathways. induced coupling reaction was applied this study peptide synthesis (SolPPS). Peptide bond formation occurred few minutes with high efficiency and no...