A5024474804- Mast cells and histamine
- Neuroscience and Neuropharmacology Research
- Ion channel regulation and function
- Phenothiazines and Benzothiazines Synthesis and Activities
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Adenosine and Purinergic Signaling
- Circadian rhythm and melatonin
- Coordination Chemistry and Organometallics
- RNA modifications and cancer
- Pain Mechanisms and Treatments
- Glioma Diagnosis and Treatment
- Synthesis and biological activity
- Epilepsy research and treatment
- Multicomponent Synthesis of Heterocycles
- Microwave-Assisted Synthesis and Applications
- Cholinesterase and Neurodegenerative Diseases
- Free Radicals and Antioxidants
- Zebrafish Biomedical Research Applications
- DNA and Nucleic Acid Chemistry
- Cardiac electrophysiology and arrhythmias
- Fluorine in Organic Chemistry
- Synthesis of heterocyclic compounds
- Synthesis and Biological Evaluation
- Polyamine Metabolism and Applications
University of Parma
2012-2024
University of Virginia Health System
2016
Weatherford College
2010-2014
Siena Biotech (Italy)
2007
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining Nav1.7 contribution to nociceptive signalling has been hampered by lack selective inhibitors. Here we report two potent and arylsulfonamide inhibitors; PF-05198007 PF-05089771, which have used directly interrogate Nav1.7’s role in nociceptor physiology. We predominant functional TTX-sensitive Nav mouse human nociceptors contributes initiation...
Dravet syndrome is caused by dominant loss-of-function mutations in SCN1A which cause reduced activity of Nav1.1 leading to lack neuronal inhibition. On the other hand, gain-of-function SCN8A can lead a severe epileptic encephalopathy subtype over activating NaV1.6 channels. These observations suggest that and Nav1.6 represent two opposing sides balance between inhibition activation. Here, we hypothesize may be treated either enhancing or reducing activity. To test this hypothesis generated...
Glioblastoma (GBM, grade IV glioma) represents the most aggressive brain tumor and patients with GBM have a poor prognosis. Until now surgical resection followed by radiotherapy temozolomide (TMZ) treatment standard strategy for GBM. We showed that imidazobenzoxazin-5-thione MV1035 is able to significantly reduce U87-MG cells migration invasiveness through inhibition of RNA demethylase ALKBH5. In this work, we focus on DNA repair protein ALKBH2, further target resulting from SPILLO-PBSS...
A simple and efficient approach to selectively obtain 2,4(5)-diarylimidazoles suppressing formation of 2-aroyl-4(5)-arylimidazoles is described. The yield each the two products strongly depends on reaction conditions employed. This provides a method prepare small libraries biologically active compounds by parallel synthesis.
Glioblastoma is an aggressive brain tumor with high mortality and a median survival of about 15 months. Starting from our previous published compound, MV1035 that inhibited migration invasiveness glioblastoma U87 cells, also exhibited synergic effect in combination the alkylating agent Temozolomide, we identified new active molecules, aim to understand key motifs responsible for activity against DNA repair protein ALKBH2 RNA demethylase ALKBH5. We modified original structure MV1035,...
A simple and efficient microwave assisted synthesis of imidazobenzoxazines, imidazobenzoxazin-5-ones, imidazobenzoxazin-5-thiones with broad chemistry scope is described. The molecules were prepared both under conventional as well heating conditions, to provide in high yields clean scalable reactions a small library imidazole-based privileged structures for drug discovery.
5-Methoxy-2-(N-acetylaminoethyl)indole (5d), a melatonin analogue derived from the transposition of acetylaminoethyl side chain C3 to C2 indole nucleus, had been previously characterized as low affinity antagonist at MT1 and MT2 membrane receptors; this molecule is endowed with good in vitro antioxidant cytoprotective potency rat cerebellar cell cultures, comparable or better than those melatonin. In order further investigate role structure-antioxidant activity relationships cytoprotection,...
The pandemic emergency determined by the spreading worldwide of SARS-CoV-2 virus has focused scientific and economic efforts pharmaceutical industry governments on possibility to fight genetic immunization. material must be delivered inside cells means vectors. Due risk adverse or immunogenic reaction replication connected with more efficient viral vectors, non-viral vectors are in many cases considered as a preferred strategy for gene delivery into eukaryotic cells. This paper is devoted...