Search results for: Simona Bertoni

Items from 1 to 20 out of 48 results

article

Mesenteric ischemia-reperfusion: an overview of preclinical drug strategies

Simona Bertoni, Vigilio Ballabeni, Elisabetta Barocelli, Massimiliano Tognolini

Drug Discovery Today > 2018 > 23 > 7 > 1416-1425

Mesenteric ischemia is a surgical emergency caused by a transient reduction in blood perfusion to the bowel. Despite accounting for only 0.1% of hospital admissions and 1–2% of gastrointestinal diseases, its elusive symptoms often lead to dramatically high morbidity and mortality rates. The complex cascade of inflammatory events and mediators triggered by mesenteric ischemia-reperfusion (I/R) accounts...

article

Tu1746 - Protection by Pharmacological Disruption of Ephb-Ephrinb System in Experimental Colitis: Tnbs-Induced vs Acute or Chronic DSS-Colitis

Irene Zini, Andrea Grandi, Valentina Vivo, Lisa Flammini, more

Gastroenterology > 2018 > 154 > 6(S1) > S-1008

article

Effects of L-DOPA/Benserazide Co-Treatment on Colonic Dysmotility and Enteric Inflammation Following Dopaminergic Nigrostriatal Neurodegeneration

Carolina Pellegrini, Luca Antonioli, Rocchina Colucci, Erika Tirotta, more

Gastroenterology > 2017 > 152 > 5(S1) > S179-S180

article

Sa1431 Intestinal Hypoxia and Reperfusion: Role for Eph-ephrin System

Valentina Vivo, Simona Bertoni, Irene Zini, Lisa Flammini, more

Gastroenterology > 2016 > 150 > 4(S1) > S313

article

Sa1839 Distinct Roles of α4β2 and α7 Nicotinic Receptors in the Modulation of Inflammatory Responses in TNBS-Induced Colitis

Andrea Grandi, Simona Bertoni, Lisa Flammini, Valentina Vivo, more

Gastroenterology > 2016 > 150 > 4(S1) > S378

article

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Eph–ephrin system

Riccardo Castelli, Massimiliano Tognolini, Federica Vacondio, Matteo Incerti, more

European Journal of Medicinal Chemistry > 2015 > 103 > C > 312-324

The Eph receptor–ephrin system is an emerging target for the development of novel anti-angiogenic therapies. Research programs aimed at developing small-molecule antagonists of the Eph receptors are still in their initial stage as available compounds suffer from pharmacological drawbacks, limiting their application in vitro and in vivo. In the present work, we report the design, synthesis and evaluation...

article

Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors

Chiara Brullo, Matteo Massa, Carla Villa, Roberta Ricciarelli, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 13 > 3426-3435

A new series of selective PDE4D inhibitors has been designed and synthesized by replacing 3-methoxy group with 3-difluoromethoxy isoster moiety in our previously reported cathecolic structures. All compounds showed a good PDE4D3 inhibitory activity, most of them being inactive toward other PDE4 isoforms (PDE4A4, PDE4B2 and PDE4C2). Compound 3b, chosen among the synthesized compounds as the most promising...

article

Mo1704 Is Eph-Ephrin Signaling Beneficial in TNBS-Induced Colitis?

Andrea Grandi, Simona Bertoni, Valentina Vivo, Massimiliano Tognolini, more

Gastroenterology > 2015 > 148 > 4(S1) > S-690

article

1,8-Naphthyridines IX. Potent anti-inflammatory and/or analgesic activity of a new group of substituted 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides, of some their Mannich base derivatives and of one novel substituted 5-amino-10-oxo-10H-pyrimido[1,2-a][1,8]naphthyridine-6-carboxamide derivative

Mario Di Braccio, Giancarlo Grossi, Silvana Alfei, Vigilio Ballabeni, more

European Journal of Medicinal Chemistry > 2014 > 86 > Complete > 394-405

A new group of 5-(alkylamino)-9-isopropyl[1,2,4]triazolo[4,3-a][1,8]naphthyridine derivatives bearing a CONHR group at the 6-position (1c–g), designed to obtain new effective analgesic and/or anti-inflammatory agents, were synthesized and tested along with three new 9-alkyl-5-(4-alkyl-1-piperazinyl)-N,N-diethyl [1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamides (2b–d). Besides, a new class of...

article

Radiological analysis of gastrointestinal dysmotility in a model of central nervous dopaminergic degeneration: Comparative study with conventional in vivo techniques in the rat

Gaia Vegezzi, Zainab Al Harraq, Giovanna Levandis, Silvia Cerri, more

Journal of Pharmacological and Toxicological Methods > 2014 > 70 > 2 > 163-169

Gastrointestinal (GI) motility disorders include many clinical manifestations associated with various pathologies. They are widespread and can be considered a primary symptom or can be associated to other diseases, such as Parkinson's disease. Understanding the type and site of GI dysmotility is crucial to identify the functional abnormality and to unravel the underlying mechanisms, in order to design...

article

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites

Fabio Del Bello, Alessandro Bonifazi, Wilma Quaglia, Angelica Mazzolari, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 15 > 3255-3259

The methyl group in cis stereochemical relationship with the basic chain of all pentatomic cyclic analogues of ACh is crucial for the agonist activity at mAChR. Among these only cevimeline (1) is employed in the treatment of xerostomia associated with Sjögren’s syndrome. Here we demonstrated that, unlike 1,3-dioxolane derivatives, in the 1,4-dioxane series the methyl group is not essential for the...

article

Bis(ammonio)alkane-type agonists of muscarinic acetylcholine receptors: Synthesis, in vitro functional characterization, and in vivo evaluation of their analgesic activity

Carlo Matera, Lisa Flammini, Marta Quadri, Valentina Vivo, more

European Journal of Medicinal Chemistry > 2014 > 75 > Complete > 222-232

In this study, we synthesized and tested in vitro and in vivo two groups of bis(ammonio)alkane-type compounds, 6a–9a and 6b–9b, which incorporate the orthosteric muscarinic agonist iperoxo into a molecular fragment of the M ₂ -selective allosteric modulators W84 and naphmethonium. The agonist potency and efficacy of these hybrid derivatives at M ₁ , M ₂ and M ₃ muscarinic...

article

Suppression of inflammatory events associated to intestinal ischemia–reperfusion by 5-HT1A blockade in mice

Simona Bertoni, Valentina Arcaro, Valentina Vivo, Alberto Rapalli, more

Pharmacological Research > 2014 > 81 > Complete > 17-25

Intestinal ischemia and reperfusion (I/R) is a potentially life-threatening disease, ensuing from various clinical conditions. Experimentally, either protective or detrimental roles have been attributed to 5-HT in the functional and morphological injury caused by mesenteric I/R. Recently, we proved the involvement of 5-HT _2A receptors in the intestinal dysmotility and leukocyte recruitment...

article

Protective role of μ opioid receptor activation in intestinal inflammation induced by mesenteric ischemia/reperfusion in mice

Francesca Saccani, Laura Anselmi, Ingrid Jaramillo, Simona Bertoni, more

Journal of Neuroscience Research > 90 > 11 > 2146 - 2153

Intestinal ischemia is a clinical emergency with high morbidity and mortality. We investigated whether activation of μ opioid receptor (μOR) protects from the inflammation induced by intestinal ischemia and reperfusion (I/R) in mice. Ischemia was induced by occlusion of the superior mesenteric artery (45 min), followed by reperfusion (5 hr). Sham‐operated (SO) and normal (N) mice served as controls...

article

Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain

Fabrizio Bordi, Silvia Rivara, Elisa Dallaturca, Caterina Carmi, more

European Journal of Medicinal Chemistry > 2012 > 48 > Complete > 214-230

Within a series of histamine H ₃ -antagonists characterized by a biphenyl core and two basic groups, we identified (S)-1-{[4′-((2-methylpyrrolidin-1-yl)methyl)biphenyl-4-yl]methyl}piperidine as a lead scaffold to introduce an additional lipophilic chain at the benzylic carbon close to the pyrrolidine ring. A series of derivatives was synthesized and tested for their binding affinity at human...

article

Ocotea quixos Lam. essential oil: In vitro and in vivo investigation on its anti-inflammatory properties

Vigilio Ballabeni, Massimiliano Tognolini, Carmine Giorgio, Simona Bertoni, more

Fitoterapia > 2010 > 81 > 4 > 289-295

Here we investigated the anti-inflammatory properties of Ocotea quixos essential oil and of its main components, trans-cinnamaldehyde and methyl cinnamate, in in vitro and in vivo models. Ocotea essential oil and trans-cinnamaldehyde but not methyl cinnamate significantly reduced LPS-induced NO release from J774 macrophages at non-toxic concentrations, inhibited LPS-induced COX-2 expression and increased...

article

W1923 Accommodation and Peristalsis are Functional Responses to Chronic Obstruction in Rat Hypertrophic Ileum

Simona Bertoni, Lisa Flammini, Francesca Saccani, Vigilio Ballabeni, more

Gastroenterology > 2010 > 138 > 5 Supplement 1 > S-766-S-767

article

T2032 Daily Assumption of Fermented Milk Containing Bifidobacterium breve 246 B® Promotes Prophylactic Effects Against Intestinal Inflammation in Mice

Paola Ghizzardi, Francesca Saccani, Gaia Vegezzi, Thomas Gobbetti, more

Gastroenterology > 2010 > 138 > 5 Supplement 1 > S-617

article

1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoid of acute gastrolesivity

Giorgio Roma, Mario Di Braccio, Giancarlo Grossi, Daniela Piras, more

European Journal of Medicinal Chemistry > 2010 > 45 > 1 > 352-366

On the basis of the very interesting pharmacological properties shown by the 5-amino[1,2,4]triazolo[4,3-a][1,8]naphthyridine-6-carboxamide derivatives 1, previously described by us, we have now prepared the 5-aminoimidazo[1,2-a][1,8]naphthyridine-6-carboxamide derivatives 2a–o (a new structural class) whose tricyclic system is isosteric to that of compounds 1. Both compounds 2 and some new properly...

article

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation

Alessandro Piergentili, Wilma Quaglia, Fabio Del Bello, Mario Giannella, more

Bioorganic & Medicinal Chemistry > 2009 > 17 > 24 > 8174-8185

Novel analogues of cis-N,N,N-trimethyl-(6-methyl-1,4-dioxan-2-yl)methanaminium iodide (2a) were synthesized by inserting methyl groups alternatively or simultaneously in positions 5 and 6 of the 1,4-dioxane nucleus in all combinations. Their biological profile was assessed by receptor binding assays at human muscarinic M ₁ –M ₅ receptors stably expressed in CHO cells and by functional...

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INFONA - science communication portal

Search results for: Simona Bertoni

Mesenteric ischemia-reperfusion: an overview of preclinical drug strategies

Tu1746 - Protection by Pharmacological Disruption of Ephb-Ephrinb System in Experimental Colitis: Tnbs-Induced vs Acute or Chronic DSS-Colitis

Effects of L-DOPA/Benserazide Co-Treatment on Colonic Dysmotility and Enteric Inflammation Following Dopaminergic Nigrostriatal Neurodegeneration

Sa1431 Intestinal Hypoxia and Reperfusion: Role for Eph-ephrin System

Sa1839 Distinct Roles of α4β2 and α7 Nicotinic Receptors in the Modulation of Inflammatory Responses in TNBS-Induced Colitis

Δ5-Cholenoyl-amino acids as selective and orally available antagonists of the Eph–ephrin system

Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors

Mo1704 Is Eph-Ephrin Signaling Beneficial in TNBS-Induced Colitis?

Radiological analysis of gastrointestinal dysmotility in a model of central nervous dopaminergic degeneration: Comparative study with conventional in vivo techniques in the rat

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites

Bis(ammonio)alkane-type agonists of muscarinic acetylcholine receptors: Synthesis, in vitro functional characterization, and in vivo evaluation of their analgesic activity

Suppression of inflammatory events associated to intestinal ischemia–reperfusion by 5-HT1A blockade in mice

Protective role of μ opioid receptor activation in intestinal inflammation induced by mesenteric ischemia/reperfusion in mice

Dibasic biphenyl H3 receptor antagonists: Steric tolerance for a lipophilic side chain

Ocotea quixos Lam. essential oil: In vitro and in vivo investigation on its anti-inflammatory properties

W1923 Accommodation and Peristalsis are Functional Responses to Chronic Obstruction in Rat Hypertrophic Ileum

T2032 Daily Assumption of Fermented Milk Containing Bifidobacterium breve 246 B® Promotes Prophylactic Effects Against Intestinal Inflammation in Mice

1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoid of acute gastrolesivity

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation

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