A5048593211- Receptor Mechanisms and Signaling
- Adenosine and Purinergic Signaling
- Pharmacological Receptor Mechanisms and Effects
- Neuropeptides and Animal Physiology
- Synthesis and Biological Evaluation
- Neuroscience and Neuropharmacology Research
- Neurotransmitter Receptor Influence on Behavior
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Eicosanoids and Hypertension Pharmacology
- Vagus Nerve Stimulation Research
- Phenothiazines and Benzothiazines Synthesis and Activities
- Phytochemicals and Antioxidant Activities
- Nicotinic Acetylcholine Receptors Study
- Nitric Oxide and Endothelin Effects
- Synthesis of heterocyclic compounds
- Synthesis and biological activity
- Bioactive Compounds and Antitumor Agents
- Antibiotics Pharmacokinetics and Efficacy
- Date Palm Research Studies
- Advanced biosensing and bioanalysis techniques
- Quinazolinone synthesis and applications
- Ion channel regulation and function
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Cholinesterase and Neurodegenerative Diseases
Università di Camerino
2016-2025
Institute of Medicinal Plant Development
2015
University of Catania
2007
University of Modena and Reggio Emilia
2005
University of Florence
2004
University of Bologna
2000-2003
We conducted a chemical and biological investigation of blue honeysuckle growing in eastern Russia.
Adenosine, a pervasive signaling molecule mediated by its interaction with G-protein-coupled receptor subtypes, especially the A2A adenosine (A2AAR), plays crucial role in cancer treatment. Recently, A2AAR targeting analogs have been proposed as potential therapeutic target for However, molecules and their mode of action inhibiting glioblastoma cell progression remain unknown. We synthesized six derivatives substituted at 9-, 2- and/or N6- 8- positions, anti-proliferative efficacy against...
Parkinson's disease (PD) represents a growing challenge to global health, as it involves millions of people. The high grade disability is due the loss dopaminergic neuron activity, and levodopa gold-standard therapy used restore dopamine in dopamine-denervated regions. Another therapeutic approach use A2A adenosine receptor antagonists and, among them, istradefylline only one currently approved for association with levodopa. In this work, we synthesized represented by...
The pathological condition of neuroinflammation is caused by the activation neuroimmune cells astrocytes and microglia. autacoid adenosine seems to be an important neuromodulator in this condition. Its main receptors involved modulation are A1AR A2AAR. Evidence suggests that produces a neuroprotective effect A2AARs block prevents neuroinflammation. aim work elucidate effects these using partial agonist 2′-dCCPA (2-chloro-N6-cyclopentyl-2′-deoxyadenosine) (C1 KiA1AR = 550 nM, KiA2AAR 24,800...
Abstract Guanosine, released extracellularly from neurons and glial cells, plays important roles in the central nervous system, including neuroprotection. The innovative DELFIA Eu‐GTP binding assay was optimized for characterization of putative guanosine receptor site at rat brain membranes by using a series novel known derivatives. These nucleosides were prepared modifying purine sugar moieties 6‐ 5′‐positions, respectively. Results these experiments prove that guanosine, 6‐thioguanosine,...
In this work, we describe the identification of 1,2,4-triazolo[4,3-a]pyrazin-3-one as a new versatile scaffold for development adenosine human (h) receptor antagonists. The chemotype ensued from molecular simplification approach applied to our previously reported 1,2,4-triazolo[4,3-a]quinoxalin-1-one series. Hence, set novel 8-amino-2-aryl-1,2,4-triazolopyrazin-3-one derivatives, featured by different substituents on 2-phenyl ring (R) and at position 6 (R6), was synthesized with main purpose...
Abstract Cerebral ischemia is the second most common cause of death and a major disability worldwide. Available therapies are based only on anticoagulants or recombinant tissue plasminogen activator. Extracellular adenosine increases during acts as neuroprotective endogenous agent mainly by activating A 1 receptors (A Rs) which control calcium influx, glutamate release, membrane potential, metabolism. Accordingly, in many experimental paradigms it has been already demonstrated that...
A series of aralkylphenoxyethylamine and aralkylmethoxyphenylpiperazine compounds was synthesized their in vitro pharmacological profile at both 5-HT1A receptors α1-adrenoceptor subtypes measured by binding assay functional studies. The results showed that the replacement 1,3-dioxolane ring a tetrahydrofuran, cyclopentanone, or cyclopentanol moiety leads to an overall reduction affinity while potency efficacy were increased receptor. significant improvement 5-HT1A/α1 selectivity observed...
Based on a screening of chemical library A2A adenosine receptor (AR) antagonists, series di- and tri-substituted adenine derivatives were synthesized tested for their ability to inhibit the activity enzyme casein kinase 1 delta (CK1δ) bind receptors (ARs). Some derivatives, here called “dual anta-inhibitors”, demonstrated good CK1δ inhibitory combined with high binding affinity, especially A2AAR. The N6-methyl-(2-benzimidazolyl)-2-dimethyamino-9-cyclopentyladenine (17, IC50 = 0.59 μM KiA2A...
A new series of 2-aralkynyl-N6-methyl-MECAs 10−13 were synthesized and evaluated in radioligand binding studies a Eu-GTP functional assay that provides powerful alternative to radioisotope use. The compounds possess high affinity selectivity for the AA3R with N6-methyl-2-phenylethynylMECA (10) showing subnanomolar about 100000-fold vs AA1R AA2AR. Furthermore, nucleosides showed be full agonists, N6-methyl-2-(2-pyridinyl)ethynylMECA (13) being most potent series.
The anticancer activity of isofuranodiene, extracted from Smyrnium olusatrum , was evaluated in human breast adenocarcinomas MDA-MB 231 and BT 474, Caucasian prostate adenocarcinoma PC 3 cell lines by MTS assay. assay showed a dose-dependent growth inhibition the tumor after isofuranodiene treatment. best antiproliferative found on cells with an IC 50 value 29 <mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML" id="M1"><mml:mrow><mml:mi>μ</mml:mi></mml:mrow></mml:math>M, which slightly...