Giuseppe Caliendo

Summary

Affiliation: Federico II University
Country: Italy

Publications

  1. ncbi request reprint A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT(1A) receptor ligands
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica di Napoli Federico II, via D Montesano, 49 80131, Napoli, Italy
    Eur J Pharm Sci 16:15-28. 2002
  2. ncbi request reprint Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT1A serotonin receptor ligands
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, Naples, Italy
    Bioorg Med Chem 8:533-8. 2000
  3. ncbi request reprint Synthesis by microwave irradiation of a substituted benzoxazine parallel library with preferential relaxant activity for guinea pig trachealis
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    Eur J Med Chem 39:815-26. 2004
  4. ncbi request reprint Derivatives as 5HT1A receptor ligands--past and present
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, via D Montesano, 49, Naples, Italy
    Curr Med Chem 12:1721-53. 2005
  5. ncbi request reprint Synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives potassium channel openers
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    Bioorg Med Chem 10:2663-9. 2002
  6. ncbi request reprint Synthesis by microwave irradiation and binding properties of novel 5-HT(1A) receptor ligands
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica di Napoli Federico II, via D Montesano, 49 80131 Naples, Italy
    Eur J Med Chem 36:873-86. 2001
  7. ncbi request reprint Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, Via Domenico Montesano 49, I 80131, Naples, Italy
    Eur J Med Chem 36:517-30. 2001
  8. ncbi request reprint Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Napoli Federico II, Napoli, Italy
    Arch Pharm (Weinheim) 341:20-7. 2008
  9. doi request reprint New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49 80131 Napoli, Italy
    Eur J Med Chem 47:520-9. 2012
  10. ncbi request reprint Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage
    Elisa Perissutti
    Dipartimento di Chimica Farmaceutica e Tossicologica and Dipartimento di Farmacologia Sperimentale, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    J Med Chem 49:7774-80. 2006

Collaborators

Detail Information

Publications44

  1. ncbi request reprint A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT(1A) receptor ligands
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica di Napoli Federico II, via D Montesano, 49 80131, Napoli, Italy
    Eur J Pharm Sci 16:15-28. 2002
    ..All compounds displayed moderate affinity for 5-HT(1A) receptor. The most interesting compound 33 showed a high affinity (K(i)=93 nM) which was combined with no affinity on the other receptors considered...
  2. ncbi request reprint Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT1A serotonin receptor ligands
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, Naples, Italy
    Bioorg Med Chem 8:533-8. 2000
    ..A o-OCH3 derivative (2e) bound at 5-HT1A sites with subnanomolar affinity (IC50 = 0.059 nM) and shows high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents...
  3. ncbi request reprint Synthesis by microwave irradiation of a substituted benzoxazine parallel library with preferential relaxant activity for guinea pig trachealis
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    Eur J Med Chem 39:815-26. 2004
    ..All N,N-dimethyl amide derivatives showed a relaxant activity higher on guinea pig trachea rings than on rat aorta rings...
  4. ncbi request reprint Derivatives as 5HT1A receptor ligands--past and present
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, via D Montesano, 49, Naples, Italy
    Curr Med Chem 12:1721-53. 2005
    ..In this review, we report an overview of the 5-HT1A receptor ligands, belonging to different chemical classes...
  5. ncbi request reprint Synthesis and vasorelaxant activity of new 1,4-benzoxazine derivatives potassium channel openers
    Giuseppe Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    Bioorg Med Chem 10:2663-9. 2002
    ..Several new 1,4-benzoxazine derivatives were provided with significant vasorelaxant activity with an overall pharmacological behavior similar to CRK (1f, 1i, 2d, 2e, 2f and 2i)...
  6. ncbi request reprint Synthesis by microwave irradiation and binding properties of novel 5-HT(1A) receptor ligands
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica di Napoli Federico II, via D Montesano, 49 80131 Naples, Italy
    Eur J Med Chem 36:873-86. 2001
    ....
  7. ncbi request reprint Synthesis of substituted benzamides as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 but do not cause gastric damage
    G Caliendo
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, Via Domenico Montesano 49, I 80131, Naples, Italy
    Eur J Med Chem 36:517-30. 2001
    ..In addition, both prevented indomethacin-induced gastric damage. Thus, these compounds may guide the definition of a new leading structure with anti-inflammatory activity that may allow designing new safer NSAIDs...
  8. ncbi request reprint Synthesis and in-vitro pharmacological evaluation of new 5-HT1A receptor ligands containing a benzotriazinone nucleus
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Napoli Federico II, Napoli, Italy
    Arch Pharm (Weinheim) 341:20-7. 2008
    ..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...
  9. doi request reprint New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49 80131 Napoli, Italy
    Eur J Med Chem 47:520-9. 2012
    ..000185nM, was the most active and selective derivative for the 5-HT(2A) receptor compared to other serotoninergic, dopaminergic and adrenergic receptors...
  10. ncbi request reprint Synthesis of 2-methyl-3-indolylacetic derivatives as anti-inflammatory agents that inhibit preferentially cyclooxygenase 1 without gastric damage
    Elisa Perissutti
    Dipartimento di Chimica Farmaceutica e Tossicologica and Dipartimento di Farmacologia Sperimentale, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    J Med Chem 49:7774-80. 2006
    ..Results showed that 3 and 4 preferentially inhibited COX-1 in vitro and in vivo. MD simulations indicated an induced fit for COX-1 but not for COX-2, probably because of a lower plasticity of the latter...
  11. doi request reprint Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Naples, Italy
    Eur J Med Chem 46:2206-16. 2011
    ....
  12. doi request reprint Efficient microwave combinatorial synthesis of novel indolic arylpiperazine derivatives as serotoninergic ligands
    Francesco Frecentese
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli, via D Montesano 49, 80131 Naples, Italy
    Eur J Med Chem 45:752-9. 2010
    ....
  13. doi request reprint New 5-HT(1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: synthesis and in vitro pharmacological evaluation
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49, 80131 Napoli, Italy
    Bioorg Med Chem Lett 20:2978-82. 2010
    ..038 nM, was the most active and selective derivative for the 5-HT(1A) receptor with respect to other serotoninergic, dopaminergic and adrenergic receptors...
  14. ncbi request reprint New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Napoli, Italy
    J Med Chem 48:5495-503. 2005
    ....
  15. ncbi request reprint Synthesis by microwave irradiation and antidiarrhoeal activity of benzotriazinone and saccharine derivatives
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita Degli Studi Di Napoli, Federico II, Napoli, Italy
    Arch Pharm (Weinheim) 338:548-55. 2005
    ..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...
  16. doi request reprint Synthesis and pharmacological evaluation of peptide-mimetic protease-activated receptor-1 antagonists containing novel heterocyclic scaffolds
    Beatrice Severino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli Federico II Via D Montesano, 49, 80131 Napoli, Italy
    Bioorg Med Chem 16:6009-20. 2008
    ..The compounds, tested on aortic rings, confirmed the results obtained in the aggregation assay...
  17. ncbi request reprint Efficient microwave combinatorial parallel and nonparallel synthesis of N-alkylated glycine methyl esters as peptide building blocks
    Vincenzo Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49, 80131 Naples, Italy
    J Comb Chem 7:618-21. 2005
    ..The described reactions are reductive alkylations of several aldehydes and glycine methyl ester in the presence of NaBH3CN. Good yields and short reaction times are the main aspects of these procedures...
  18. doi request reprint Synthesis of benzamide derivatives and their evaluation as antiprion agents
    Ferdinando Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Napoli, Italy
    Bioorg Med Chem 20:5001-11. 2012
    ..The results clearly indicate the benzamide derivatives as attractive lead compounds for the development of potential therapeutic agents against prion disease...
  19. ncbi request reprint Minimal structural requirements for agonist activity of PAR-2 activating peptides
    Vincenzo Santagada
    Department of Pharmaceutical Chemistry, University of Naples Federico II, via D Montesano 49, 80131, Naples, Italy
    Bioorg Med Chem Lett 12:21-4. 2002
    ..Our study resulted in the discovery of dipeptide derivatives of N(alpha)-benzoyl-Arg(NO(2))-Leu-NH(2) displaying a potency comparable to that of the full-length rat PAR-2 activating peptide (Ser-Leu-Ile-Gly-Arg-Leu-NH(2))...
  20. ncbi request reprint 5-HT1A Receptor: An Old Target as a New Attractive Tool in Drug Discovery from Central Nervous System to Cancer
    Ferdinando Fiorino
    Dipartimento di Farmacia, Universita degli Studi di Napoli Federico II, via D Montesano, 49, 80131, Napoli, Italy
    J Med Chem 57:4407-26. 2014
    ..This aspect could be really interesting to consider and justify the 5-HT1A receptor as a new attractive target for drug discovery. ..
  21. ncbi request reprint Identification of a pepducin acting as S1P3 receptor antagonist
    Beatrice Severino
    Dipartimento di Farmacia, Universita di Napoli Federico II, via D Montesano, 49, 80131, Napoli, Italy
    J Pept Sci 19:717-24. 2013
    ..These results suggested a correlation between specific conformations and activities...
  22. ncbi request reprint Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors
    Vincenzo Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano 49, 80131 Napoli, Italy
    J Med Chem 49:1882-90. 2006
    ..To rationalize the obtained results, molecular modeling experiments were carried out suggesting the molecular basis of FTase inhibition by these products...
  23. ncbi request reprint Synthesis and in vitro pharmacological evaluation of a new series of 5-HT1A 5-HT2A and 5-HT2C receptor ligands containing a norbornene nucleus
    F Fiorino
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita degli Studi di Napoli Federico II, Napoli, Italy
    Pharmazie 64:555-64. 2009
    ..Moreover, compound 3p showed mixed 5-HT2A/5-HT2C activity with affinity values in nanomolar range...
  24. ncbi request reprint A suitable 1,2,4-oxadiazoles synthesis by microwave irradiation
    Vincenzo Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, via D Montesano, 49, 80131 Naples, Italy
    Bioorg Med Chem Lett 14:4491-3. 2004
    ..Good yields and short reaction times were the main aspects of the methods...
  25. ncbi request reprint Peptide T revisited: conformational mimicry of epitopes of anti-HIV proteins
    D Picone
    Dipartimento di Chimica, Universita degli Studi di Napoli Federico II, Complesso Universitario di Monte S Angelo, Italy
    J Pept Sci 7:197-207. 2001
    ....
  26. ncbi request reprint Probing the shape of a hydrophobic pocket in the active site of delta-opioid antagonists
    V Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, Universita di Napoli Federico II, Italy
    J Pept Sci 7:374-85. 2001
    ..Accordingly, it is possible to use the shape of the different side chains to map the hydrophobic cavity of the receptor. The resulting complementary image is funnel shaped...
  27. ncbi request reprint The application of microwave irradiation as new convenient synthetic procedure in drug discovery
    V Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, via D Montesano, 49, Naples, Italy
    Curr Med Chem 9:1251-83. 2002
    ..In addition we report some of the most recently disclosed applications in combinatorial chemistry...
  28. ncbi request reprint Microwave assisted synthesis: a new technology in drug discovery
    V Santagada
    Dipartimento di Chimica Farmaceutica e Tossicologica, via D Montesano, 49, 80131 Naples, Italy
    Mini Rev Med Chem 9:340-58. 2009
    ....
  29. doi request reprint Neurounina-1, a novel compound that increases Na+/Ca2+ exchanger activity, effectively protects against stroke damage
    Pasquale Molinaro
    Division of Pharmacology, Department of Neuroscience, School of Medicine, Federico II University of Naples, Via Pansini 5, 80131 Naples, Italy
    Mol Pharmacol 83:142-56. 2013
    ..Collectively, the present study shows that neurounina-1 exerts a remarkable neuroprotective effect during stroke and increases NCX1 and NCX2 activities...
  30. ncbi request reprint The nitric oxide related therapeutic phenomenon: a challenging task
    Giuseppe Cirino
    Dipartimento di Farmacologia Sperimentale, Via Domenico Montesano, 49, 80131 Napoli, Italy
    Curr Pharm Des 8:233-9. 2002
    ..This review will briefly addresses some of the major areas of biology where NO has been involved and give an overview of what is the state of the art in developing drugs that works through NO...
  31. ncbi request reprint Evidence for a protective role played by the Na+/Ca2+ exchanger in cerebral ischemia induced by middle cerebral artery occlusion in male rats
    Giuseppe Pignataro
    Department of Neuroscience, Division of Pharmacology, University of Naples, Federico II Via S Pansini 5, 80131 Naples, Italy
    Neuropharmacology 46:439-48. 2004
    ..These results suggest that a stimulation of NCX activity may help neurons and glial cells that are not irreversibly damaged in the penumbral zone to survive, whereas its pharmacological blockade can compromise their survival...
  32. ncbi request reprint Effect of positive charge in VIP 16gamma-glutamyl diamino derivatives on hVPAC1 and hVPAC2 receptor function
    Salvatore De Maria
    Department of Experimental Medicine, Medical School, II University of Naples, Via Costantinopoli 16, 80138, Naples, Italy
    J Pept Sci 14:102-9. 2008
    ....
  33. ncbi request reprint Synthesis of 6beta-D-glucosyl and 6-nitroxy (-)-galanthamine derivatives as acetylcholinesterase inhibitors
    E Perissutti
    Dipartimento di Chimica Farmaceutica e Tossicologica1, Universita di Napoli Federico II, Napoli, Italy
    Pharmazie 62:403-5. 2007
    ..Compounds 2, 3 and 5 presented a percentage of inhibition of 35.22%, 47.48% and 67.89% respectively...
  34. ncbi request reprint Recent advances in synthesis of PAR ligands as therapeutic strategy for inflammatory diseases
    B Severino
    Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, via D Montesano 49, 80131 Naples, Italy
    Mini Rev Med Chem 9:653-63. 2009
    ..This mini-review will focus on recent advances in the synthesis of PAR ligands highlighting their therapeutic potential in the treatment of various inflammatory diseases...
  35. ncbi request reprint Synthesis of novel anti-inflammatory peptides derived from the amino-acid sequence of the bioactive protein SV-IV
    A Ialenti
    Department of Experimental Pharmacology, Faculty of Pharmacy, University of Naples Federico II, Naples, Italy
    Eur J Biochem 268:3399-406. 2001
    ....
  36. ncbi request reprint Na+/Ca2+ exchanger in Na+ efflux-Ca2+ influx mode of operation exerts a neuroprotective role in cellular models of in vitro anoxia and in vivo cerebral ischemia
    A Tortiglione
    Division of Pharmacology, Department of Neuroscience, School of Medicine, Federico II University of Naples, 80131 Naples, Italy
    Ann N Y Acad Sci 976:408-12. 2002
  37. doi request reprint Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction
    Haroldo A Flores Toque
    Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas, Campinas, Brazil
    J Med Chem 51:2807-15. 2008
    ..Because several analogues were significantly more lipophilic than sildenafil, these compounds may offer a new lead for development of new sildenafil analogues...
  38. ncbi request reprint Sequence and structure-activity relationship of a scorpion venom toxin with nitrergic activity in rabbit corpus cavernosum
    Cleber E Teixeira
    Department of Pharmacology, Faculty of Medical Sciences, UNICAMP, Campinas SP, 13081 970, Brazil
    FASEB J 17:485-7. 2003
    ....
  39. ncbi request reprint PAR1 antagonism protects against experimental liver fibrosis. Role of proteinase receptors in stellate cell activation
    Stefano Fiorucci
    Dipartimento di Medicina Clinica, Patologia, Clinica di Gastroenterologia ed Endoscopia Digestiva, University of Perugia, Perugia
    Hepatology 39:365-75. 2004
    ..In conclusion, PAR(s) regulates HSC activity; development of PAR antagonists might be a feasible therapeutic strategy for protecting against fibrosis in patients with chronic liver diseases...
  40. ncbi request reprint 5-Amino-2-hydroxybenzoic acid 4-(5-thioxo-5H-[1,2]dithiol-3yl)-phenyl ester (ATB-429), a hydrogen sulfide-releasing derivative of mesalamine, exerts antinociceptive effects in a model of postinflammatory hypersensitivity
    Eleonora Distrutti
    Clinica di Gastroenterologia, Policlinico Monteluce, University of Perugia, Via Enrico Dal Pozzo, 06122 Perugia, Italy
    J Pharmacol Exp Ther 319:447-58. 2006
    ..This study provides evidence that H(2)S-releasing drugs might have beneficial effects in the treatment of painful intestinal disorders...
  41. ncbi request reprint Pharmacokinetic profile of atenolol aspirinate
    Ana C Montes-Gil
    Department of Pharmacology, Faculty of Medical Sciences, State University of Campinas, Campinas, Sao Paulo, Brazil
    Arch Pharm (Weinheim) 340:445-55. 2007
    ..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...
  42. ncbi request reprint Gastrointestinal safety and anti-inflammatory effects of a hydrogen sulfide-releasing diclofenac derivative in the rat
    John L Wallace
    Inflammation Research Network, University of Calgary, 3330 Hospital Drive NW, Calgary, Alberta, Canada
    Gastroenterology 132:261-71. 2007
    ..In this study, we evaluated the gastrointestinal safety and anti-inflammatory effects of a novel "HS-NSAID" (ATB-337) that consists of diclofenac linked to a hydrogen sulfide-releasing moiety...
  43. ncbi request reprint Conformation-activity relationship of peptide T and new pseudocyclic hexapeptide analogs
    Annamaria D'ursi
    Dipartimento di Scienze Farmaceutiche, Universita di Salerno, 84084 Fisciano Italy
    J Pept Sci 13:413-21. 2007
    ..No low-energy models could be derived starting from the type-II beta-turn conformation of peptide T. The analogs with the most favored conformations are also the most active in the chemotactic test...
  44. ncbi request reprint Design of inhibitors for human tissue kallikrein using non-natural aromatic and basic amino acids
    Daniel C Pimenta
    Department of Biophysics, Escola Paulista de Medicina, Universidade Federal de Sao Paulo, SP, Brazil
    Biol Chem 383:853-7. 2002
    ..Finally, we present a series of peptides that were assayed as competitive inhibitors for human tissue kallikrein that may lead to the development of novel peptides, which are both more potent and selective...