Gilberto Spadoni

Gilberto Spadoni

UNVERIFIED PROFILE

Are you Gilberto Spadoni?   Register this Author

Register author
Gilberto Spadoni

Gilberto Spadoni

Publications by authors named "Gilberto Spadoni"

Are you Gilberto Spadoni?   Register this Author

56Publications

667Reads

39Profile Views

New Antimicrobials Targeting Bacterial RNA Polymerase Holoenzyme Assembly Identified with an BRET-Based Discovery Platform.

ACS Chem Biol 2019 Aug 30;14(8):1727-1736. Epub 2019 Jul 30.

Laboratory of Biochemistry and Molecular Biology, Department of Chemistry, Life Sciences and Environmental Sustainability , University of Parma , 43124 Parma , Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acschembio.9b00178DOI Listing
August 2019

Melatonin MT and MT Receptors Exhibit Distinct Effects in the Modulation of Body Temperature across the Light/Dark Cycle.

Int J Mol Sci 2019 May 17;20(10). Epub 2019 May 17.

Neurobiological Psychiatry Unit, Department of Psychiatry, McGill University Health Center (MUHC), McGill University, Montreal, QC H3A1A1, Canada.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms20102452DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6566544PMC
May 2019

Design, Synthesis, and Biological Activity of Hydrogen Peroxide Responsive Arylboronate Melatonin Hybrids.

Chem Res Toxicol 2019 01 3;32(1):100-112. Epub 2019 Jan 3.

Department of Biomolecular Sciences , University of Urbino Carlo Bo , Piazza Rinascimento 6 , I-61029 Urbino , Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.chemrestox.8b00216DOI Listing
January 2019

Tetrahydroquinoline Ring as a Versatile Bioisostere of Tetralin for Melatonin Receptor Ligands.

J Med Chem 2018 04 4;61(8):3726-3737. Epub 2018 Apr 4.

Dipartimento di Scienze Biomolecolari , Università degli Studi di Urbino "Carlo Bo" , Piazza Rinascimento 6 , I-61029 Urbino , Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.jmedchem.8b00359DOI Listing
April 2018

Antiproliferative and pro-apoptotic activity of melatonin analogues on melanoma and breast cancer cells.

Oncotarget 2017 Sep 10;8(40):68338-68353. Epub 2017 Aug 10.

Department of Medical Biotechnology and Translational Medicine, Università degli Studi di Milano, Milan, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.18632/oncotarget.20124DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5620261PMC
September 2017

Pharmacokinetic and pharmacodynamic evaluation of ramelteon : an insomnia therapy.

Expert Opin Drug Metab Toxicol 2015 Jul 8;11(7):1145-56. Epub 2015 May 8.

Università degli Studi di Urbino "Carlo Bo", Dipartimento di Scienze Biomolecolari , Piazza Rinascimento 6, I-61029 Urbino , Italy +039 0722 303322 ; +039 0722 303313 ;

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1517/17425255.2015.1045487DOI Listing
July 2015

Therapeutic uses of melatonin and melatonin derivatives: a patent review (2012 - 2014).

Expert Opin Ther Pat 2015 Apr 12;25(4):425-41. Epub 2015 Jan 12.

Università degli Studi di Parma, Dipartimento di Farmacia , Parco Area delle Scienze 27/A, I-43124 Parma , Italy +39 0521 905061 ; +39 0521 905006 ;

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1517/13543776.2014.1001739DOI Listing
April 2015

Iridium-catalyzed direct synthesis of tryptamine derivatives from indoles: exploiting n-protected β-amino alcohols as alkylating agents.

J Org Chem 2015 Mar 26;80(6):3217-22. Epub 2015 Feb 26.

Department of Biomolecular Sciences, University of Urbino "Carlo Bo", Piazza del Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/acs.joc.5b00195DOI Listing
March 2015

Selective melatonin MT2 receptor ligands relieve neuropathic pain through modulation of brainstem descending antinociceptive pathways.

Pain 2015 Feb;156(2):305-17

aNeurobiological Psychiatry Unit, Department of Psychiatry, McGill University Health Centre, McGill University, Montreal, QC, Canada bInstitute of Neuroethology, University Veracruzana, Xalapa, México cDepartment of Experimental Medicine, Second University of Naples, Naples, Italy dInstitute of Life Sciences, Scuola Superiore Sant'Anna, Pisa, Italy eDepartment of Pharmacology, Chemotherapy and Medical Toxicology, University of Milan, Milan, Italy fInstitute of Medicinal Chemistry, University Carlo Bo, Urbino, Italy gNeurobiology of Pain Laboratory, Department of Pharmacobiology, Cinvestav-Sede Sur, México, D. F., Mexico.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1097/01.j.pain.0000460311.71572.5fDOI Listing
February 2015

Synthesis and characterization of new bivalent agents as melatonin- and histamine H3-ligands.

Int J Mol Sci 2014 Sep 12;15(9):16114-33. Epub 2014 Sep 12.

Dipartimento di Scienze Biomolecolari, Università degli Studi di Urbino "Carlo Bo", Piazza Rinascimento 6, I-61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms150916114DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4200786PMC
September 2014

Synthesis of 2-substituted tryptophans via a C3- to C2-alkyl migration.

Beilstein J Org Chem 2014 26;10:1991-8. Epub 2014 Aug 26.

Department of Biomolecular Sciences, University of Urbino "Carlo Bo", Piazza del Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3762/bjoc.10.207DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168769PMC
September 2014

Towards the development of 5-HT₇ ligands combining serotonin-like and arylpiperazine moieties.

Eur J Med Chem 2014 Jun 13;80:8-35. Epub 2014 Apr 13.

Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Italy. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2014.04.034DOI Listing
June 2014

Melatonin, selective and non-selective MT1/MT2 receptors agonists: differential effects on the 24-h vigilance states.

Neurosci Lett 2014 Feb 7;561:156-61. Epub 2014 Jan 7.

Neurobiological Psychiatry Unit, Department of Psychiatry, McGill University Health Center, McGill University, Montreal, QC, Canada. Electronic address:

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.neulet.2013.12.069DOI Listing
February 2014

Homology models of melatonin receptors: challenges and recent advances.

Int J Mol Sci 2013 Apr 12;14(4):8093-121. Epub 2013 Apr 12.

Dipartimento di Farmacia, Università degli Studi di Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.3390/ijms14048093DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3645733PMC
April 2013

Anxiolytic effects of the melatonin MT(2) receptor partial agonist UCM765: comparison with melatonin and diazepam.

Prog Neuropsychopharmacol Biol Psychiatry 2012 Dec 10;39(2):318-25. Epub 2012 Jul 10.

Neurobiological Psychiatry Unit, Department of Psychiatry, McGill University and McGill University Health Center, Montreal, QC, Canada.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.pnpbp.2012.07.003DOI Listing
December 2012

Synthesis of tryptamine derivatives via a direct, one-pot reductive alkylation of indoles.

J Org Chem 2012 Jul 3;77(14):6351-7. Epub 2012 Jul 3.

Department of Biomolecular Sciences, University of Urbino, Piazza Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jo3010028DOI Listing
July 2012

Melatonin receptor agonists: new options for insomnia and depression treatment.

CNS Neurosci Ther 2011 Dec;17(6):733-41

Dipartimento di Scienze del Farmaco e della Salute, University of Urbino Carlo Bo, Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1111/j.1755-5949.2010.00197.xDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6493855PMC
December 2011

Bivalent ligand approach on N-{2-[(3-methoxyphenyl)methylamino]ethyl}acetamide: synthesis, binding affinity and intrinsic activity for MT(1) and MT(2) melatonin receptors.

Bioorg Med Chem 2011 Aug 28;19(16):4910-6. Epub 2011 Jun 28.

Dipartimento di Scienze Biomolecolari, Università degli Studi di Urbino Carlo Bo, Piazza Rinascimento 6, 61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2011.06.063DOI Listing
August 2011

ST1936 stimulates cAMP, Ca2+, ERK1/2 and Fyn kinase through a full activation of cloned human 5-HT6 receptors.

Eur J Pharmacol 2011 Jul 28;661(1-3):8-14. Epub 2011 Apr 28.

Sigma-tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejphar.2011.04.028DOI Listing
July 2011

Direct, one-pot reductive alkylation of anilines with functionalized acetals mediated by triethylsilane and TFA. Straightforward route for unsymmetrically substituted ethylenediamine.

J Org Chem 2011 Jan 22;76(2):704-7. Epub 2010 Dec 22.

Department of Drug and Health Sciences, University of Urbino Carlo Bo, Piazza del Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jo102109fDOI Listing
January 2011

A novel one-pot approach of hexahydropyrrolo[2,3-b]indole nucleus by a cascade addition/cyclization strategy: synthesis of (+/-)-esermethole.

Org Lett 2010 Sep;12(17):3844-7

Department of Drug and Health Sciences, University of Urbino Carlo Bo, Piazza del Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/ol101527jDOI Listing
September 2010

Recent advances in the development of melatonin MT(1) and MT(2) receptor agonists.

Expert Opin Ther Pat 2010 Aug;20(8):1059-77

Dipartimento Farmaceutico, Università degli Studi di Parma, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1517/13543776.2010.496455DOI Listing
August 2010

Melatonin receptor agonists: SAR and applications to the treatment of sleep-wake disorders.

Curr Top Med Chem 2008 ;8(11):954-68

Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G. P. Usberti 27/A, Campus Universitario, 43100 Parma, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.2174/156802608784936719DOI Listing
October 2008

An improved synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT): a selective MT(2) melatonin receptor antagonist.

Org Biomol Chem 2008 Jan 13;6(1):147-50. Epub 2007 Nov 13.

Institute of Medicinal Chemistry, University of Urbino "Carlo Bo", Piazza del Rinascimento 6, 61029 Urbino (PU), Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1039/b713904gDOI Listing
January 2008

N-(substituted-anilinoethyl)amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands.

J Med Chem 2007 Dec 6;50(26):6618-26. Epub 2007 Dec 6.

Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G. P. Usberti 27/A, Campus Universitario, 43100 Parma, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm700957jDOI Listing
December 2007

Synthesis and biological activity of new melatonin dimeric derivatives.

Bioorg Med Chem 2007 Jul 30;15(13):4643-50. Epub 2007 Mar 30.

Istituto di Chimica Farmaceutica, Università degli Studi di Urbino Carlo Bo, 61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2007.03.080DOI Listing
July 2007

Design and synthesis of N-(3,3-diphenylpropenyl)alkanamides as a novel class of high-affinity MT2-selective melatonin receptor ligands.

J Med Chem 2006 Dec;49(25):7393-403

Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino Carlo Bo, Piazza Rinascimento 6, 61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm060850aDOI Listing
December 2006

Towards the development of mixed MT(1)-agonist/MT(2)-antagonist melatonin receptor ligands.

ChemMedChem 2006 Oct;1(10):1099-105

Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino Carlo Bo, Piazza Rinascimento 6, Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/cmdc.200600133DOI Listing
October 2006

Application of 3D-QSAR in the rational design of receptor ligands and enzyme inhibitors.

Chem Biodivers 2005 Nov;2(11):1438-51

Dipartimento Farmaceutico, Università degli Studi di Parma, Parco Area delle 27/A, I-43100 Parma.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1002/cbdv.200590117DOI Listing
November 2005

Synthesis and conformational study of 3,4-carbocyclic bridged indole melatonin and serotonin analogues.

Bioorg Med Chem 2005 Aug;13(15):4651-7

Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino Carlo Bo, Piazza Rinascimento 6, I-61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2005.04.064DOI Listing
August 2005

Antioxidant and cytoprotective activity of indole derivatives related to melatonin.

Adv Exp Med Biol 2003 ;527:567-75

Dipartimento Farmaceutico, Università degli Studi di Parma, Parco Area delle Scienze 27/a, I-43100 Parma.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/978-1-4615-0135-0_65DOI Listing
September 2004

Strategies leading to MT2 selective melatonin receptor antagonists.

Adv Exp Med Biol 2003 ;527:577-85

Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino, Piazza Rinascimento 6, I-61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1007/978-1-4615-0135-0_66DOI Listing
September 2004

Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.

J Med Chem 2004 Aug;47(17):4202-12

Dipartimento di Farmacologia, Chemioterapia e Tossicologia Medica, Università degli Studi di Milano, Via Vanvitelli 32, I-20129 Milano, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm040768kDOI Listing
August 2004

Synthesis and structure-activity relationships of a series of pyrrole cannabinoid receptor agonists.

Bioorg Med Chem 2003 Sep;11(18):3965-73

Istituto di Chimica Farmaceutica e Tossicologica, Università degli Studi di Urbino Carlo Bo, Piazza del Rinascimento 6, I-61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1016/s0968-0896(03)00413-9DOI Listing
September 2003

The hypnotic and analgesic effects of 2-bromomelatonin.

Anesth Analg 2003 Sep;97(3):763-8

Department of Anesthesia, University of Iowa College of Medicine, Iowa City, Iowa, USA.

View Article

Download full-text PDF

Source
http://dx.doi.org/10.1213/01.ane.0000074796.10856.1fDOI Listing
September 2003

Conformation by NMR of two tetralin-based receptor ligands.

Farmaco 2003 Jul;58(7):469-76

Istituto di Chimica Farmaceutica, Università degli Studi di Urbino, Piazza Rinascimento 6, I-61029 Urbino, Italy.

View Article

Download full-text PDF

Source
http://linkinghub.elsevier.com/retrieve/pii/S0014827X0300064
Publisher Site
http://dx.doi.org/10.1016/S0014-827X(03)00064-8DOI Listing
July 2003

Effects of melatonin and melatonin receptors ligand N-[(4-methoxy-1H-indol-2-yl)methyl]propanamide on murine Colon 38 cancer growth in vitro and in vivo.

Neuro Endocrinol Lett 2002 Apr;23 Suppl 1:50-4

Department of Experimental Endocrinology and Hormone Diagnostics, Institute of Endocrinology, Medical University of Lodz, Lodz, Poland.

View Article

Download full-text PDF

Source
April 2002