A5069752323- Peroxisome Proliferator-Activated Receptors
- Nitric Oxide and Endothelin Effects
- Synthesis and biological activity
- Adipose Tissue and Metabolism
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Catalytic Reactions
- Enzyme function and inhibition
- Sirtuins and Resveratrol in Medicine
- Synthesis and Biological Evaluation
- Analytical Chemistry and Chromatography
- Cholinesterase and Neurodegenerative Diseases
- Protein Degradation and Inhibitors
- Bioactive Compounds and Antitumor Agents
- Metabolism, Diabetes, and Cancer
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Estrogen and related hormone effects
- Organic Chemistry Cycloaddition Reactions
- Computational Drug Discovery Methods
- Histone Deacetylase Inhibitors Research
- Cancer, Hypoxia, and Metabolism
- Phenothiazines and Benzothiazines Synthesis and Activities
- Genomics, phytochemicals, and oxidative stress
- Click Chemistry and Applications
- Sulfur-Based Synthesis Techniques
University of Chieti-Pescara
2015-2024
Ospedale SS. Annunziata
2016
Istituto di Farmacologia Traslazionale
2015
Istituto di Metodologie Chimiche
2006
Vibrio cholerae causes life-threatening infections in low-income countries due to the rise of antibacterial resistance. Innovative pharmacological targets have been investigated and carbonic anhydrases (CAs, EC: 4.2.1.1) encoded by V. (VchCAs) emerged as a valuable option. Recently, we developed large library para- meta-benzenesulfonamides characterised moieties with different flexibility degree CAs inhibitors. Stopped flow-based enzymatic assays showed strong inhibition VchαCA for this...
Aim: Development of dual-acting antibacterial agents containing Erlotinib, a recognized EGFR inhibitor used as an anticancer agent, with differently spaced benzenesulfonamide moieties known to bind and inhibit Helicobacter pylori carbonic anhydrase (HpCA) or the antiviral Zidovudine. Methods & materials: Through rational design, ten derivatives were obtained via straightforward synthesis including click chemistry reaction. Inhibitory activity against panel pathogenic anhydrases...
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...
Neurodegenerative diseases (NDs) are described as multifactorial and progressive syndromes with compromised cognitive behavioral functions. The multi-target-directed ligand (MTDL) strategy is a promising paradigm in drug discovery, potentially leading to new opportunities manage such complex diseases. Here, we studied the dual ability of set resveratrol (RSV) analogs inhibit two important targets involved neurodegeneration. stilbenols 1−9 were tested inhibitors human monoamine oxidases...
Immunotherapy has marked a revolution in cancer therapy. The most extensively studied target this field is represented by the protein-protein interaction between PD-1 and its ligand, PD-L1. promising results obtained with clinical use of monoclonal antibodies (mAbs) directed against both PD-L1 have prompted search for small-molecule binders capable disrupting contact overcoming limitations presented mAbs. disclosure first X-ray complexes BMS ligands showed protein dimeric form, ligand...
Herein we report a first study on single molecular entities bearing both Epidermal Growth Factor Receptor (EGFR) and Carbonic Anhydrase (CA) Inhibiting moieties as new tools for the management of...
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...
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)...
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...