List of works - Antimo Gioiello

Achiral-chiral two-dimensional chromatography of free amino acids in milk: A promising tool for detecting different levels of mastitis in cows.

scientific article published on 3 January 2015

Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators

scientific article

BF(3).Et(2)O-induced decomposition of ethyl 2-diazo-3-hydroxy-3,3-diarylpropanoates in acetonitrile: a novel approach to 2,3-diaryl beta-enamino ester derivatives.

scientific article

Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.

scientific article published on July 2006

Chromatographic separation of free dafachronic acid epimers with a novel triazole click quinidine-based chiral stationary phase

scientific article published on 06 March 2014

Continuous Flow Synthesis of Thieno[2,3-c]isoquinolin-5(4H)-one Scaffold: A Valuable Source of PARP-1 Inhibitors

Continuous flow synthesis and scale-up of glycine- and taurine-conjugated bile salts

scientific article published on 19 April 2012

Correlation between CMC and chromatographic index: simple and effective evaluation of the hydrophobic/hydrophilic balance of bile acids

scientific article published on 16 June 2007

D-leucine microparticles as an excipient to improve the aerosolization performances of dry powders for inhalation

scientific article published on 21 January 2019

Derived chromatographic indices as effective tools to study the self-aggregation process of bile acids

scientific article published on 06 November 2008

Determination of bile salt critical micellization concentration on the road to drug discovery

scientific article published on 04 July 2013

Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.

scientific article published in December 2009

Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases

scientific article published on 15 June 2015

Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool

scientific article published on 24 June 2019

Enantioselective HPLC Analysis to Assist the Chemical Exploration of Chiral Imidazolines

scientific article published on 02 February 2020

Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists

scientific article published on 27 December 2018

Exploring the Synthetic Versatility of the Lewis Acid Induced Decomposition Reaction of α-Diazo-β-hydroxy Esters. The Case of Ethyl Diazo(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)acetate

scientific article published on 17 August 2011

Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.

scientific article

First general approach to cyclohex-3-ene-1,1-bis(phosphonates) by Diels-Alder cycloaddition of tetraethyl vinylidenebis(phosphonate) to 1,3-dienes.

scientific article

Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors

scientific article published on 04 June 2014

Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor

scientific article published on 20 March 2020

Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs-Knorr reaction optimization

scientific article published on 23 October 2014

HPLC/ELSD analysis of amidated bile acids: an effective and rapid way to assist continuous flow chemistry processes

scientific article published on 10 August 2012

Identification and quantification of oxo-bile acids in human faeces with liquid chromatography-mass spectrometry: A potent tool for human gut acidic sterolbiome studies

scientific article published on 19 November 2018

Investigating the allosteric reverse signalling of PARP inhibitors with microsecond molecular dynamic simulations and fluorescence anisotropy

scientific article published on 22 July 2014

Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.

scientific article

Molecular dynamics simulation of the ligand binding domain of farnesoid X receptor. Insights into helix-12 stability and coactivator peptide stabilization in response to agonist binding

scientific article published on 01 May 2005

Molecular field analysis and 3D-quantitative structure-activity relationship study (MFA 3D-QSAR) unveil novel features of bile acid recognition at TGR5.

scientific article published on 13 August 2008

Multiclass screening method to detect more than fifty banned substances in bovine bile and urine

scientific article published on 14 June 2018

Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies

scientific article

Novel stereoselective synthesis and chromatographic evaluation of E-guggulsterone

scientific article published on 03 December 2011

Patented TGR5 modulators: a review (2006 - present).

scientific article published on 06 October 2012

Probing the Binding Site of Bile Acids in TGR5.

scientific article

Progress and challenges of selective Farnesoid X Receptor modulation

scientific article published on 20 June 2018

Selected cholesterol biosynthesis inhibitors produce accumulation of the intermediate FF-MAS that targets nucleus and activates LXRα in HepG2 cells.

scientific article published on 9 May 2017

Semisynthetic bile acid FXR and TGR5 agonists: physicochemical properties, pharmacokinetics, and metabolism in the rat

scientific article published on 01 May 2014

Side-chain modified bile acids: chromatographic separation of 23-methyl epimers

scientific article published on 01 June 2009

Steroids interfere with human carbonic anhydrase activity by using alternative binding mechanisms

scientific article published on 01 December 2018

Synthesis and quantitative structure-property relationships of side chain-modified hyodeoxycholic acid derivatives.

scientific article published on 30 August 2013

Synthesis and structure-activity relationships of amino acid conjugates of cholanic acid as antagonists of the EphA2 receptor.

scientific article published on 21 October 2013

Synthesis of atypical bile acids for use as investigative tools for the genetic defect of 3β-hydroxy-Δ(5)-C27-steroid oxidoreductase deficiency

scientific article published on 19 June 2014

Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.

scientific article published on 11 December 2017

TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading

scientific article

TGR5-mediated bile acid sensing controls glucose homeostasis

scientific article

Tandem mass spectrometric determination of atypical 3β-hydroxy-Δ5-bile acids in patients with 3β-hydroxy-Δ5-C27-steroid oxidoreductase deficiency: application to diagnosis and monitoring of bile acid therapeutic response

article

The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology

scientific article published on 21 February 2020

List of works by Antimo Gioiello

Achiral-chiral two-dimensional chromatography of free amino acids in milk: A promising tool for detecting different levels of mastitis in cows.

Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators

BF(3).Et(2)O-induced decomposition of ethyl 2-diazo-3-hydroxy-3,3-diarylpropanoates in acetonitrile: a novel approach to 2,3-diaryl beta-enamino ester derivatives.

Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives.

Chromatographic separation of free dafachronic acid epimers with a novel triazole click quinidine-based chiral stationary phase

Continuous Flow Synthesis of Thieno[2,3-c]isoquinolin-5(4H)-one Scaffold: A Valuable Source of PARP-1 Inhibitors

Continuous flow synthesis and scale-up of glycine- and taurine-conjugated bile salts

Correlation between CMC and chromatographic index: simple and effective evaluation of the hydrophobic/hydrophilic balance of bile acids

D-leucine microparticles as an excipient to improve the aerosolization performances of dry powders for inhalation

Derived chromatographic indices as effective tools to study the self-aggregation process of bile acids

Determination of bile salt critical micellization concentration on the road to drug discovery

Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.

Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases

Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool

Enantioselective HPLC Analysis to Assist the Chemical Exploration of Chiral Imidazolines

Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists

Exploring the Synthetic Versatility of the Lewis Acid Induced Decomposition Reaction of α-Diazo-β-hydroxy Esters. The Case of Ethyl Diazo(3-hydroxy-2-oxo-2,3-dihydro-1H-indol-3-yl)acetate

Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.

First general approach to cyclohex-3-ene-1,1-bis(phosphonates) by Diels-Alder cycloaddition of tetraethyl vinylidenebis(phosphonate) to 1,3-dienes.

Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors

Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor

Glucuronidation of bile acids under flow conditions: design of experiments and Koenigs-Knorr reaction optimization

HPLC/ELSD analysis of amidated bile acids: an effective and rapid way to assist continuous flow chemistry processes

Identification and quantification of oxo-bile acids in human faeces with liquid chromatography-mass spectrometry: A potent tool for human gut acidic sterolbiome studies

Investigating the allosteric reverse signalling of PARP inhibitors with microsecond molecular dynamic simulations and fluorescence anisotropy

Lead Discovery of Dual G-Quadruplex Stabilizers and Poly(ADP-ribose) Polymerases (PARPs) Inhibitors: A New Avenue in Anticancer Treatment.

Molecular dynamics simulation of the ligand binding domain of farnesoid X receptor. Insights into helix-12 stability and coactivator peptide stabilization in response to agonist binding

Molecular field analysis and 3D-quantitative structure-activity relationship study (MFA 3D-QSAR) unveil novel features of bile acid recognition at TGR5.

Multiclass screening method to detect more than fifty banned substances in bovine bile and urine

Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies

Novel stereoselective synthesis and chromatographic evaluation of E-guggulsterone

Patented TGR5 modulators: a review (2006 - present).

Probing the Binding Site of Bile Acids in TGR5.

Progress and challenges of selective Farnesoid X Receptor modulation

Selected cholesterol biosynthesis inhibitors produce accumulation of the intermediate FF-MAS that targets nucleus and activates LXRα in HepG2 cells.

Semisynthetic bile acid FXR and TGR5 agonists: physicochemical properties, pharmacokinetics, and metabolism in the rat

Side-chain modified bile acids: chromatographic separation of 23-methyl epimers

Steroids interfere with human carbonic anhydrase activity by using alternative binding mechanisms

Synthesis and quantitative structure-property relationships of side chain-modified hyodeoxycholic acid derivatives.

Synthesis and structure-activity relationships of amino acid conjugates of cholanic acid as antagonists of the EphA2 receptor.

Synthesis of atypical bile acids for use as investigative tools for the genetic defect of 3β-hydroxy-Δ(5)-C27-steroid oxidoreductase deficiency

Synthesis, physicochemical properties, and biological activity of bile acids 3-glucuronides: Novel insights into bile acid signalling and detoxification.

TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading

TGR5-mediated bile acid sensing controls glucose homeostasis

Tandem mass spectrometric determination of atypical 3β-hydroxy-Δ5-bile acids in patients with 3β-hydroxy-Δ5-C27-steroid oxidoreductase deficiency: application to diagnosis and monitoring of bile acid therapeutic response

The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology

Thermal and catalytic reactions of ethyl diazopyruvate with [60]fullerene