A5062948323- Peroxisome Proliferator-Activated Receptors
- Adipose Tissue and Metabolism
- Nitric Oxide and Endothelin Effects
- Synthesis and biological activity
- Synthesis and Catalytic Reactions
- Eicosanoids and Hypertension Pharmacology
- Sirtuins and Resveratrol in Medicine
- Metabolism, Diabetes, and Cancer
- Analytical Chemistry and Chromatography
- Chemical Synthesis and Analysis
- Synthesis and Biological Evaluation
- Enzyme function and inhibition
- Bioactive Compounds and Antitumor Agents
- Click Chemistry and Applications
- Estrogen and related hormone effects
- Receptor Mechanisms and Signaling
- Protein Degradation and Inhibitors
- Organic Chemistry Cycloaddition Reactions
- Sulfur-Based Synthesis Techniques
- Asymmetric Synthesis and Catalysis
- Cholinesterase and Neurodegenerative Diseases
- Piperaceae Chemical and Biological Studies
- Nuclear Receptors and Signaling
- Electron Spin Resonance Studies
- Neuroscience and Neuropharmacology Research
University of Chieti-Pescara
2015-2024
Italian National Agency for the Evaluation of Universities and Research Institutes
2023
Istituto di Farmacologia Traslazionale
2015
The high incidence and mortality of invasive fungal infections serious drug resistance have become a global public health issue. There is an urgent need for alternative antimicrobials to control targeting it by antifungal substances from the natural sources represents promising new strategy development novel agents. Resveratrol (3,5,4'-trihydroxy-trans-stilbene) phytoalexin produced plant species in response environmental stress or pathogenic attacks. It has many known potential therapeutic...
This study explores the limitations and benefits of different approaches to conducting online focus groups illustrates an group protocol used within Value for Schools project in Italy. According evaluation design, 13 were organized, with participation 101 teachers 37 school principals. The setup, incorporation, reorganization indications have been discussed literature, addressing methodological practical issues, such as selection participants preliminary communication them; web conference...
A library of sulfonate and sulfonamide derivatives Resveratrol was synthesized tested for its aromatase inhibitory potential. Interestingly, were found to be more active than bioisosteres with IC50 values in the low micromolar range. The analogues 1b-c 1j exhibited good vitro antiproliferative activity on MCF7 cell line, evidenced by MTT LDH release assays. Structure-activity relationships suggested that electronic lipophilic properties could have a different role promoting biological...
Abstract Nitric oxide (NO) is an essential endogenous mediator with a physiological role in the central nervous system as neurotransmitter and neuromodulator. A growing number of studies have demonstrated that abnormal nitrergic signaling crucial event development neurodegeneration. In particular, uncontrolled production NO by neuronal nitric synthase (nNOS) observed several neurodegenerative diseases. Moreover, it well recognized specific isoforms human carbonic anhydrase (hCA)...
N-[(3-Aminomethyl)benzyl]acetamidine derivatives were synthesized and in vitro evaluated as inhibitors of the inducible isoform nitric oxide synthase (iNOS). Because high potency action excellent selectivity over endothelial (eNOS), compound 10 was ex vivo on isolated perfused resistance arteries. The results confirm that selectively inhibits iNOS, without affecting isoform. outcome docking studies showed hydrophobic interaction is driving force binding process, especially for where pocket...
The development of PPARα/γ dual or PPARα/γ/δ pan-agonists could represent an efficacious approach for a simultaneous pharmacological intervention on carbohydrate and lipid metabolism. Two series new phenyldiazenyl fibrate derivatives GL479, previously reported agonist, were synthesized tested. Compound 12a was identified as PPAR pan-agonist with moderate balanced activity the three isoforms (α, γ, δ). Moreover, docking experiments showed that adopts different binding mode in PPARγ compared...
New acetamidines structurally related to N-(3-(aminomethyl)benzyl)acetamidine (1, W1400) were designed as inhibitors of inducible nitric oxide synthase (iNOS). Six compounds found be selective for iNOS over endothelial (eNOS), and among them, the most active compound was N-benzylacetamidine 2. A docking study also performed shed light on effects structural modifications interaction with NOS.
Candida albicans represents the most prevalent microbial population in mucosal and systemic infections, usually confined to severely immunocompromised people. Considering increase of resistant strains demand for new antifungal drugs endowed with innovative mechanism action, we performed a ligand-based virtual screening order identify anti-Candida compounds. Starting from large library natural/semisynthetic products several published synthesized compounds, three coumarin derivatives were...