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11 results on '"Caliendo, Giuseppe"'

1. Synthesis, docking studies, and pharmacological evaluation of 2‐hydroxypropyl‐4‐arylpiperazine derivatives as serotoninergic ligands

Author

Magli, Elisa, primary, Kędzierska, Ewa, additional, Kaczor, Agnieszka A., additional, Bielenica, Anna, additional, Severino, Beatrice, additional, Gibuła‐Tarłowska, Ewa, additional, Kotlińska, Jolanta H., additional, Corvino, Angela, additional, Sparaco, Rosa, additional, Esposito, Giovanna, additional, Albrizio, Stefania, additional, Perissutti, Elisa, additional, Frecentese, Francesco, additional, Leśniak, Anna, additional, Bujalska‐Zadrożny, Magdalena, additional, Struga, Marta, additional, Capasso, Raffaele, additional, Santagada, Vincenzo, additional, Caliendo, Giuseppe, additional, and Fiorino, Ferdinando, additional

Published
2021
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2. Synthesis, docking studies, and pharmacological evaluation of 5HT 2C ligands containing the N ′‐cyanoisonicotinamidine or N ′‐cyanopicolinamidine nucleus

Author

Magli, Elisa, primary, Kędzierska, Ewa, additional, Kaczor, Agnieszka A., additional, Severino, Beatrice, additional, Corvino, Angela, additional, Perissutti, Elisa, additional, Frecentese, Francesco, additional, Saccone, Irene, additional, Massarelli, Paola, additional, Gibuła‐Tarłowska, Ewa, additional, Kotlińska, Jolanta H., additional, Santagada, Vincenzo, additional, Caliendo, Giuseppe, additional, and Fiorino, Ferdinando, additional

Published
2019
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4. Synthesis andIn VitroPharmacological Evaluation of Novel 2-Hydroxypropyl-4-arylpiperazine Derivatives as Serotoninergic Ligands

Author

Fiorino, Ferdinando, primary, Magli, Elisa, additional, Severino, Beatrice, additional, Corvino, Angela, additional, Ciano, Antonio, additional, Perissutti, Elisa, additional, Frecentese, Francesco, additional, Massarelli, Paola, additional, Nencini, Cristina, additional, Santagada, Vincenzo, additional, and Caliendo, Giuseppe, additional

Published
2014
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6. Pharmacokinetic Profile of Atenolol Aspirinate

Author

Montes-Gil, Ana C., primary, Zanfolin, Marcos, additional, Okuyama, Cristina E., additional, Lilla, Sergio, additional, Alves, Delma P., additional, Santagada, Vincenzo, additional, Perissutti, Elisa, additional, Lavecchia, Antonio, additional, Fiorino, Ferdinando, additional, Severino, Beatrice, additional, Caliendo, Giuseppe, additional, Priviero, Fernanda B. M., additional, Mendes, Gustavo D., additional, Donato, Jose L., additional, and Nucci, Gilberto de, additional

Published
2007
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9. Pharmacokinetic profile of atenolol aspirinate

Author

José L. Donato, Beatrice Severino, Giuseppe Caliendo, Fernanda B.M. Priviero, Elisa Perissutti, Ferdinando Fiorino, Gilberto De Nucci, Ana C. Montes-Gil, Sergio Lilla, Antonio Lavecchia, Marcos Zanfolin, Vincenzo Santagada, Delma Pegolo Alves, Cristina E. Okuyama, Gustavo D. Mendes, A. C., MONTES GIL, M., Zanfolin, C. E., Okuyama, S., Lilla, D. P., Alve, Santagada, Vincenzo, Perissutti, Elisa, Lavecchia, Antonio, Fiorino, Ferdinando, Severino, Beatrice, Caliendo, Giuseppe, F. B. M., Priviero, G. D., Mende, J. L., Donato, and G., DE NUCCIA

Subjects
Models, Molecular, Pharmaceutical Science, Hydrolysis, chemistry.chemical_compound, Pharmacokinetics, Drug Discovery, medicine, Organic chemistry, Animals, Humans, Prodrugs, cardiovascular diseases, pharmacokinetic studie, Microwaves, Antihypertensive Agents, Aqueous solution, Chromatography, Aspirin, Chemistry, molecular modeling, Mutagenicity Tests, Prodrug, Atenolol, microwave sinthesi, Gastric Mucosa, Area Under Curve, Salicylic acid, Derivative (chemistry), circulatory and respiratory physiology, medicine.drug, Half-Life
Abstract

We report microwave-assisted synthetic routes, the pharmacokinetic profile along with results from ulcerogenicity and mutagenicity studies of atenolol aspirinate, and an already described derivative, in which acetyl salicylic acid (aspirin®) was connected to atenolol by an ester linkage. Atenolol aspirinate was stable towards aqueous hydrolysis but rapidly hydrolyzed in plasma (t 1/2 = 7.6 min). The results showed that the rapid and complete hydrolysis generates atenolol salicylate, which assumes a conformation stabilized by two intramolecular H-bonds, avoiding its further hydrolysis to salicylic acid and atenolol.

Published
2007

10. Synthesis by microwave irradiation and antidiarrhoeal activity of benzotriazinone and saccharine derivatives

Author

Vincenzo Santagada, Elisa Perissutti, Ferdinando Fiorino, Angelo A. Izzo, Raffaele Capasso, Beatrice Severino, Barbara Preziosi, Giuseppe Caliendo, Francesco Frecentese, Fiorino, Ferdinando, Caliendo, Giuseppe, Perissutti, Elisa, Severino, Beatrice, Frecentese, Francesco, B., Preziosi, Izzo, ANGELO ANTONIO, Capasso, Raffaele, and Santagada, Vincenzo

Subjects
medicine.drug_class, Chemistry, Pharmaceutical, Guinea Pigs, Pharmaceutical Science, In Vitro Techniques, Chemical synthesis, Mice, Structure-Activity Relationship, Saccharin, Ileum, Drug Discovery, Antidiarrhoeal, medicine, Organic chemistry, Animals, Antidiarrheals, Gastrointestinal Transit, Microwaves, Mice, Inbred ICR, Bicyclic molecule, Molecular Structure, Chemistry, Triazines, Muscle, Smooth, General Medicine, Electric Stimulation, Benzene derivatives, Microwave irradiation, Microwave, Nuclear chemistry, Muscle Contraction
Abstract

The synthesis by microwave irradiation and the biological results of novel benzotriazinone and saccharine derivatives with potential antidiarrhoeal activity is described. Conventional and microwave heatings were compared for the reactions. Good yields and short reaction times are the main advantages of our synthetic route. Among the tested compounds, compound 12 inhibited motility both in in-vitro and in-vivo tests.

Published
2005

11. Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus.

Author

Fiorino F, Severino B, De Angelis F, Perissutti E, Frecentese F, Massarelli P, Bruni G, Collavoli E, Santagada V, and Caliendo G

Subjects
Animals, Binding Sites, Cerebral Cortex metabolism, Corpus Striatum metabolism, In Vitro Techniques, Ligands, Male, Microwaves, Naphthalenes chemistry, Naphthalenes pharmacology, Piperazines chemistry, Piperazines pharmacology, Radioligand Assay, Rats, Rats, Sprague-Dawley, Structure-Activity Relationship, Triazines chemistry, Triazines pharmacology, Naphthalenes chemical synthesis, Piperazines chemical synthesis, Receptor, Serotonin, 5-HT1A metabolism, Triazines chemical synthesis
Abstract

This paper reports the microwave-assisted synthesis and the binding assays on the 5-HT(1A), 5-HT(2A) and 5-HT(2C) receptors of new benzotriazinone derivatives, in order to identify selective ligands for the 5-HT(1A) subtype receptor. Conventional and microwave heating of the reactions were compared. Good yields and short reaction times are the main advantages of our synthetic route. More active compounds were selected and further evaluated for their binding affinities on D(1), D(2) dopaminergic and alpha(1), alpha(2) adrenergic receptors. The 3-(2-(4-(naphthalen-1-yl)piperazin-1-yl)ethyl)benzo[d][1,2,3]triazin-4(3H)-one 5 with K(i)= 0.000178 nM was the most active and selective derivative for the 5-HT(1A)receptor with respect to other serotonin receptors and the most selective derivative compared to dopaminergic and adrenergic receptors.

Published
2008
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