List of works by Gilberto Spadoni

1-(2-Alkanamidoethyl)-6-methoxyindole derivatives: a new class of potent indole melatonin analogues

scientific article published in June 1997

1-Aminocylopropane-1-carboxylic acid derivatives as ligands at the glycine-binding site of the N-methyl-D-aspartate receptor

scientific article published in March 1998

2-Bromomelatonin: synthesis and characterization of a potent melatonin agonist.

scientific article published in January 1992

2-N-acylaminoalkylindoles: design and quantitative structure-activity relationship studies leading to MT2-selective melatonin antagonists

scientific article published on August 2001

2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.

scientific article published on September 1998

3-(2-Carbamoylvinyl)-4,5-dimethylpyrrole-2-carboxylic acids as ligands at the NMDA glycine-binding site: a study on the 2-carbamoylvinyl chain modification

scientific article

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

scientific article published on September 2010

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

scientific article published on 13 November 2007

Analogues of benzamide as poly(ADP-ribose)transferase inhibitors: a study on structure activity relationships

scientific article published on 01 July 1988

Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models

scientific article published on June 2005

Antidepressant-like activity and cardioprotective effects of fatty acid amide hydrolase inhibitor URB694 in socially stressed Wistar Kyoto rats

scientific article

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

scientific article

Application of 3D-QSAR in the Rational Design of Receptor Ligands and Enzyme Inhibitors

scientific article published on 01 November 2005

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

scientific article published on 28 June 2011

Cardioprotective effects of fatty acid amide hydrolase inhibitor URB694, in a rodent model of trait anxiety.

scientific article

Chiral Recognition of Flexible Melatonin Receptor Ligands Induced by Conformational Equilibria

scientific article published on 04 September 2020

Conformation by NMR of two tetralin-based receptor ligands

scientific article

Conformationally restrained melatonin analogues: synthesis, binding affinity for the melatonin receptor, evaluation of the biological activity, and molecular modeling study

scientific article published in June 1997

Description of the constitutive activity of cloned human melatonin receptors hMT(1) and hMT(2) and discovery of inverse agonists

scientific article

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

scientific article

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

scientific article published on 03 January 2019

Diastereo- and enantioselective hydrogenation of a challenging enamide derived from 4-phenyl-2-tetralone: an appealing shortcut towards enantiopure cis-2-aminotetraline derivatives

scientific article published in March 2010

Direct, One-Pot Reductive Alkylation of Anilines with Functionalized Acetals Mediated by Triethylsilane and TFA. Straightforward Route for Unsymmetrically Substituted Ethylenediamine

scientific article published on 22 December 2010

Identification of Bivalent Ligands with Melatonin Receptor Agonist and Fatty Acid Amide Hydrolase (FAAH) Inhibitory Activity That Exhibit Ocular Hypotensive Effect in the Rabbit

scientific article published on 04 September 2018

Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities

scientific article published in March 2004

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

scientific article published on 26 February 2015

MT1-selective melatonin receptor ligands: synthesis, pharmacological evaluation, and molecular dynamics investigation of N-{[(3-O-substituted)anilino]alkyl}amides.

scientific article

Melatonin antagonizes apoptosis via receptor interaction in U937 monocytic cells

scientific article published on 01 September 2007

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

scientific article

Melatonin receptor agonists: new options for insomnia and depression treatment

scientific article published on December 2011

Melatonin receptor ligands: synthesis of new melatonin derivatives and comprehensive comparative molecular field analysis (CoMFA) study

scientific article published in September 1998

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

scientific article published on 7 January 2014

N-(Anilinoethyl)amides: design and synthesis of metabolically stable, selective melatonin receptor ligands

scientific article published in October 2009

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

scientific article

N-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition

scientific article published on 26 March 2020

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

scientific article published on 30 July 2019

New classes of potent heparanase inhibitors from ligand-based virtual screening

scientific article published on 01 December 2020

Pharmacokinetic and pharmacodynamic evaluation of ramelteon : an insomnia therapy

scientific article published on 08 May 2015

Promotion of non-rapid eye movement sleep and activation of reticular thalamic neurons by a novel MT2 melatonin receptor ligand

scientific journal article

Reassessing the melatonin pharmacophore--enantiomeric resolution, pharmacological activity, structure analysis, and molecular modeling of a constrained chiral melatonin analogue

scientific article published on 20 January 2006

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

scientific article published on August 2010

Structural requirements for inhibitors of poly(ADP-ribose) Polymerase

scientific article published on 01 January 1990

Synthesis and biological activity of new melatonin dimeric derivatives

scientific article published on 30 March 2007

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

scientific article published on 12 September 2014

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand 4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone.

scientific article published on 18 November 2011

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

scientific article published in August 2005

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

scientific article published in September 2003

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

scientific article published on 26 August 2014

Synthesis of Tryptamine Derivatives via a Direct, One-Pot Reductive Alkylation of Indoles

scientific article published on 03 July 2012

Synthesis, antioxidant activity and structure-activity relationships for a new series of 2-(N-acylaminoethyl)indoles with melatonin-like cytoprotective activity.

scientific article published in April 2006

Synthesis, enantiomeric resolution, and structure-activity relationship study of a series of 10,11-dihydro-5H-dibenzo[a,d]cycloheptene MT2 receptor antagonists

scientific article published on December 2007

Synthesis, pharmacological characterization and QSAR studies on 2-substituted indole melatonin receptor ligands.

scientific article published on April 2001

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

scientific article published on 29 March 2018

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

scientific article

Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.

scientific article published in April 2003

Toward the definition of stereochemical requirements for MT2-selective antagonists and partial agonists by studying 4-phenyl-2-propionamidotetralin derivatives

scientific article published on 18 November 2011

Towards the Development of Mixed MT1-Agonist/MT2-Antagonist Melatonin Receptor Ligands

article

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

scientific article published on 13 April 2014

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

scientific article