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3. Synthesis of phenylpyrimidinones as guanylyl cyclase C inhibitors

Author

Magli, E, Fiorino, F, Severino, B, Corvino, A, Perissutti, E, Frecentese, F, Giordano, F, Saccone, I, Luciano, P, Zaminelli, T, Santagada, V, Caliendo, G, de Nucci, G, Magli, E, Fiorino, F, Severino, B, Corvino, A, Perissutti, E, Frecentese, F, Giordano, F, Saccone, I, Luciano, P, Zaminelli, T, Santagada, V, Caliendo, G, and de Nucci, G

Abstract

Diarrhea is one of the most important causes of mortality in the developing world, being responsible for 2.5 million deaths each year. Many of these deaths are caused by enterotoxigenic strains of bacteria, like Escherichia coli, that produce enterotoxins that cause acute watery diarrhea, commonly defined as secretory diarrhea. Studies on symptomatic patients indicate a high prevalence of enterotoxigenic E. coli strains producing the heat-stable toxin, STa. STa is a small, cysteine-rich peptide that binds to the extracellular receptor domain of guanylyl cyclase C (GCC), located at the luminal membrane of intestinal epithelial cells. GCC and its endogenous peptide ligands, guanylin and uroguanylin, play a key role in balancing water absorption and hydration of the intestinal lumen, as exemplified by the finding that loss of GCC function causes severe dehydration of the intestinal lumen, culminating in intestinal obstruction. From a mechanistic viewpoint, reduction of GCC activity offers an efficient approach to limit enterotoxigenic E. coli- provoked secretory diarrhea. Inhibition of GCC-mediated cGMP production would not only reduce anion secretion, but would also restore NHE3 activity, resulting in a comprehensive antidiarrheal action. In the present study, two novel phenylpyrimidinone derivatives were simultaneously synthesized and tested for their ability to block STa-induced CFTR activity in T84 cells.

Published
2019

5. Synthesis and activity of antiflammin

Author

Salvadori, S., primary, Marastoni, M., additional, Balboni, G., additional, Scaranari, V., additional, Santagada, V., additional, Romualdi, P., additional, Ferri, S., additional, and Tomatis, R., additional

Published
1991
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7. Valutazione degli effetti di una terapia antibiotica dopo l’estrazione di terzi molari inclusi mandibolari. Studio caso-controllo Evaluation of the effects of an antibiotic therapy after extraction of impacted mandibular third molars. A case-control

Author

Bonacina, C, Santagada, V, Alciati, M, Lomartire, G, CARINI, FABRIZIO, Bonacina, C, Santagada, V, Alciati, M, Lomartire, G, and Carini, F

Subjects
terapia antibiotica,terzi molari inclusi,mandibola, MED/28 - MALATTIE ODONTOSTOMATOLOGICHE
Published
2012

9. Synthesis and in vitro pharmacological evaluation of novel 2-hydroxypropyl-4-arylpiperazine derivatives as serotoninergic ligands

Author

Fiorino, F, Magli, E, Severino, B, Corvino, A, Ciano, A, Perissutti, E, Frecentese, F, Massarelli, Paola, Nencini, Cristina, Santagada, V, Caliendo, G., Fiorino, Ferdinando, Magli, Elisa, Severino, Beatrice, Corvino, Angela, Ciano, Antonio, Perissutti, Elisa, Frecentese, Francesco, Paola, Massarelli, Cristina, Nencini, Santagada, Vincenzo, and Caliendo, Giuseppe

Subjects
Male, Serotonin, Molecular Structure, exo-N-Hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2, 5-HT1A receptor ligands, Norbornene nucleu, Arylpiperazine derivative, 5-HT1A receptor ligand, Arylpiperazine derivatives,exo-N-Hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide,5-HT1A receptor ligands,Norbornene nucleus,Serotonin, Brain, Receptors, Adrenergic, alpha, Ligands, Piperazines, Receptors, Dopamine, Rats, Sprague-Dawley, Radioligand Assay, Structure-Activity Relationship, Arylpiperazine derivatives, 3-dicarboximide, Drug Design, Receptors, Serotonin, Norbornene nucleus, Animals, Protein Binding
Abstract

This paper reports the synthesis of new norbornene and exo-N-hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide derivatives and their binding to the 5-HT1A , 5-HT2A , and 5-HT2C receptors, in order to identify selective ligands for these 5-hydroxytryptamine (5-HT, serotonine) receptor subtypes. The combination of structural elements (heterocyclic nucleus, hydroxyalkyl chain, and 4-substituted piperazine) known to be critical for affinity to 5-HT1A receptors and the proper selection of substituents led to compounds with high specificity and affinity toward serotoninergic receptors. The most active compounds were selected and further evaluated for their binding affinities to D1 , D2 dopaminergic and α1 , α2 adrenergic receptors. 4-[3-[4-(2-Furoyl)piperazin-1-yl]propoxy-2-ol]-4-aza-tricyclo[5.2.1.02,6]dec-8-ene-3,5-dione 3e with Ki = 5.04 ± 0.227 nM was the most active and selective derivative for the 5-HT2C receptor with respect to other serotonin receptors, and the most selective derivative versus dopaminergic and adrenergic receptors.

Published
2014

10. Protease activated receptor-2 activation improves efficiency of experimental ischemic precondotioning

Author

NAPOLI C, DE NIGRIS F, WALLACE J. L, CALIENDO G, CONDORELLI M, SANTAGADA V, CIRINO, GIUSEPPE, CICALA, CARLA, Napoli, C, DE NIGRIS, F, Cicala, Carla, Wallace, J. L., Caliendo, G, Condorelli, M, Santagada, V, and Cirino, Giuseppe

Subjects
myocardial ischemia, protease activated receptor 2, rat
Abstract

Protease-activated receptor-2 (PAR-2) is a member of seven transmembrane domain G protein-coupled receptors activated by proteolytic cleavage. PAR-2 is involved in inflammatory events and cardiac ischemic reperfusion injury. The objective of this study was to investigate the effects of PAR-2 in experimental myocardial ischemic preconditioning. To monitor the effects of PAR-2, Langendorff-perfused rat hearts were used. These hearts were treated with PAR-2-activating peptide (PAR-2AP) in various protocols. Hemodynamic parameters (left ventricular developed pressure, left ventricular diastolic pressure, coronary flow rate, and heart rate), several indexes of oxidative injury, and neutrophil accumulation were evaluated. We show for the first time that enhanced PAR-2 activation improves efficiency of ischemic preconditioning and reduces cardiac inflammation in the rat heart. Indeed, after PAR-2AP infusion we found that hemodynamic parameters, oxidative injury, infarct size, and neutrophil accumulation were involved. These data support the concept that PAR-2-dependent cell trafficking may regulate signaling responses to cardiac ischemia and inflammation.

Published
2002

11. Anti-inflammatory peptides: an update and future perspective

Author

SANTAGADA V, METAFORA S, CALIENDO G, MAFFIA P, MORELLI F, DE ROSA R, DE MARIA G, CARTENI' M., IALENTI, ARMANDO, Cartenì M, Santagada, V, Ialenti, Armando, Metafora, S, Caliendo, G, Maffia, P, Morelli, F, DE ROSA, R, DE MARIA, G, and Carteni', M.

Published
2002

15. Effect of positive charge in VIP (16)gamma-glutamyl diamino derivatives on hVPAC1 and hVPAC2 receptor function

Author

De Maria S, Metafora V, Metafora S, Ravagnan G, Carteni M, Pontoni G, Facchiano A, Lepretti M, Severino B, Caliendo G, Santagada V, Langer I, and Robberecht P.

Subjects
hormones, hormone substitutes, and hormone antagonists
Abstract

Increase of VPAC receptor s binding to the (16)gamma-glutamyl diaminopropane vasoactive intestinal peptide (VIP-DAP) agonist, a vasoactive intestinal polypeptide (VIP) structural analogue containing a positive charge at position 16, has confirmed the importance of a positive charge at this site. By investigating the effect of distance from the peptide backbone Calpha of a positive charge in position 16, data are reported here concerning: (i) a novel chemical method used for the synthesis of a new family of (16)gamma-glutamyl diamine VIP derivatives differing among them for single carbon atoms and including diaminoethane (VIP-DAE2), diaminopropane (VIP-DAP3), diaminobutane (VIP-DAB4), diaminopentane (VIP-DAP5), and diaminohexane (VIP-DAH6); (ii) functional characterization of these compounds on human VPAC1 and VPAC2 receptors. In more detail, the EC50 and IC50 values, when measured as a function of the alkylic chain length, show in more detail, that the use of VIP-DAB4 derivative changes the IC50 but not the EC50, thus indicating on hVPAC2 receptor an unexpected relationship between binding and activity that differs from that obtained on hVPAC1.

Published
2008

25. Synthesis and neurokinin antagonist activity of 2-benzylidene- and 2- benzyl-3-benzylamino quinuclidines

Author

Giuseppe Caliendo, Greco, G., Perissutti, E., Santagada, V., Silipo, C., Vittoria, A., Turbanti, L., Renzetti, A. R., Benedetti, E., Pedone, C., Santini, A., Caliendo, Giuseppe, Greco, Giovanni, Perissutti, Elisa, Santagada, Vincenzo, Silipo, C., Vittoria, A., Turbanti, L., Renzetti, A. R., Benedetti, E., Pedone, C., and Santini, A.

Subjects
Models, Molecular, Dose-Response Relationship, Drug, substance P, Biphenyl Compounds, Guinea Pigs, Molecular Sequence Data, quinuclidine derivative, Receptors, Neurokinin-3, Stereoisomerism, Receptors, Neurokinin-2, Crystallography, X-Ray, receptor subtype, Rats, Neurokinin-1 Receptor Antagonists, Animals, Amino Acid Sequence
Abstract

Molecular modeling studies based on the potent NK-1 antagonist CP-96,345 led us to the identification of some 2-benzylidene- and 2-benzyl-3- benzylaminoquinuclidine derivatives as potential antagonists at the NK receptor subtypes. The synthesized compounds, whose Z/E isomerism has been defined by X-ray analysis, show only moderate potency on the three neurokinin receptors. The possible reasons of the low potency exhibited by the tested compounds are discussed.

Published
1993

38. Synthesis of phenylpyrimidinones as guanylyl cyclase C inhibitors

Author

Magli, E., Fiorino, F., Severino, B., Corvino, A., Perissutti, E., Frecentese, F., Giordano, F., Saccone, I., Luciano, P., Zaminelli, T., Santagada, V., Caliendo, G., and Nucci, G. de

Abstract

Diarrhea is one of the most important causes of mortality in the developing world, being responsible for 2.5 million deaths each year. Many of these deaths are caused by enterotoxigenic strains of bacteria, likeEscherichia coli,that produce enterotoxins that cause acute watery diarrhea, commonly defined as secretory diarrhea. Studies on symptomatic patients indicate a high prevalence of enterotoxigenicE. colistrains producing the heat-stable toxin, STa. STa is a small, cysteine-rich peptide that binds to the extracellular receptor domain of guanylyl cyclase C (GCC), located at the luminal membrane of intestinal epithelial cells. GCC and its endogenous peptide ligands, guanylin and uroguanylin, play a key role in balancing water absorption and hydration of the intestinal lumen, as exemplified by the finding that loss of GCC function causes severe dehydration of the intestinal lumen, culminating in intestinal obstruction. From a mechanistic viewpoint, reduction of GCC activity offers an efficient approach to limit enterotoxigenicE. coli– provoked secretory diarrhea. Inhibition of GCC-mediated cGMP production would not only reduce anion secretion, but would also restore NHE3 activity, resulting in a comprehensive antidiarrheal action. In the present study, two novel phenylpyrimidinone derivatives were simultaneously synthesized and tested for their ability to block STa-induced CFTR activity in T84 cells.

Published
2019
Full Text
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