List of works - Roberto Di Santo

(Thiazol-2-yl)hydrazone derivatives from acetylpyridines as dual inhibitors of MAO and AChE: synthesis, biological evaluation and molecular modeling studies

scientific article published on 25 September 2015

1-Arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors

article

2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assays

scientific article published on January 2004

2H-Pyrrolo[3,4-b] [1,5]benzothiazepine derivatives as potential inhibitors of HIV-1 reverse transcriptase

scientific article

6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach

scientific article published on 5 November 2013

6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitro

scientific article

6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays

scientific article published in April 2004

A rational approach to predict and modulate stereolability of chiral alpha substituted ketones

scientific article published in January 2009

Activity of caffeic acid derivatives against Candida albicans biofilm.

scientific article published on 13 February 2014

Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies

scientific article

Antifungal agents. 11. N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole: synthesis, anti-Candida activity, and QSAR studies

scientific article published in August 2005

Antimycobacterial pyrroles: synthesis, anti-Mycobacterium tuberculosis activity and QSAR studies.

scientific article published in June 2000

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 1).

scientific article published on December 2006

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 2).

scientific article published on December 2006

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

scientific article

Biochemical characterization of a multi-drug resistant HIV-1 subtype AG reverse transcriptase: antagonism of AZT discrimination and excision pathways and sensitivity to RNase H inhibitors.

scientific article published on 4 February 2016

Cinnamoyl Compounds as Simple Molecules that Inhibit p300 Histone Acetyltransferase

scientific article published on 10 March 2007

Comparison of different methods for the extraction of cannabinoids from cannabis

scientific article published on 29 April 2019

Competing sigmatropic shift rearrangements in excited allyl radicals.

scientific article

Convenient Route to 2H-Pyrrolo[3,4-b]quinolin-9(4H)-one Skeleton via TosMIC Reaction

Conversion of a racemic mixture of 8-chloro-2-(2,6-difluorophenylmethyl)-2,3-dihydro-3-methyl-1,2,5-benzothiadiazepin-4(5h)-one 1,1-dioxide into a single enantiomer via a chromatographic resolution/racemization method.

scientific article published in May 2003

Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents

scientific article published on 23 January 2019

Design, synthesis and QSAR studies on N-aryl heteroarylisopropanolamines, a new class of non-peptidic HIV-1 protease inhibitors

scientific article

Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors

scientific article published on 11 February 2014

Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors

scientific article published in June 2005

Design, synthesis, and structure-activity relationship of N-arylnaphthylamine derivatives as amyloid aggregation inhibitors

scientific article published in October 2012

Design, synthesis, biological evaluation, and molecular modeling studies of TIBO-like cyclic sulfones as non-nucleoside HIV-1 reverse transcriptase inhibitors

scientific article published on January 2006

Development of a human immunodeficiency virus vector-based, single-cycle assay for evaluation of anti-integrase compounds

scientific article

Diaryl Disulfides as Novel Stabilizers of Tumor Suppressor Pdcd4

scientific article

Diketo Acids Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and the Reverse Transcriptase RNase H Domain ⬇️

scientific article published on January 1, 2011

Diketo hexenoic acid derivatives are novel selective non-nucleoside inhibitors of mammalian terminal deoxynucleotidyl transferases, with potent cytotoxic effect against leukemic cells

scientific article

Discovery and Pharmacological Profile of New 1H-Indazole-3-carboxamide and 2H-Pyrrolo[3,4-c]quinoline Derivatives as Selective Serotonin 4 Receptor Ligands

scientific article published on 24 October 2012

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

scientific article published on 22 June 2015

Discovery of in vitro antitubercular agents through in silico ligand-based approaches.

scientific article

Effects of polyphenol compounds on influenza A virus replication and definition of their mechanism of action

scientific article

Enantioselective liquid chromatography of C3-chiral 2,3-dihydro-1,2,5-benzothiadiazepin-4(5H)-one and thione 1,1-dioxides on polyacrylamide- and polysaccharide-based chiral stationary phases ⬇️

scientific article published on April 18, 2003

Evaluation of HIV-1 integrase inhibitors on human primary macrophages using a luciferase-based single-cycle phenotypic assay.

scientific article

Evaluation of the Anti-<i>Histoplasma capsulatum</i> Activity of Indole and Nitrofuran Derivatives and Their Pharmacological Safety in Three-Dimensional Cell Cultures

scientific article published on 12 May 2022

Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans.

scientific article published on November 2016

Geometrically and conformationally restrained cinnamoyl compounds as inhibitors of HIV-1 integrase: synthesis, biological evaluation, and molecular modeling.

scientific article published on October 1998

HIV-1 RT-Associated RNase H Function Inhibitors: Recent Advances in Drug Development ⬇️

scientific article published on January 1, 2010

HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein

scientific article

Human immunodeficiency virus type 1 (HIV-1) integration: a potential target for microbicides to prevent cell-free or cell-associated HIV-1 infection

scientific article published on 12 May 2008

Human terminal deoxynucleotidyl transferases as novel targets for anticancer chemotherapy

scientific article published on January 2006

Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats

scientific article published on 16 February 2015

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

scientific article

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives

scientific article

In Vitro Antiviral Activity of New Oxazoline Derivatives as Potent Poliovirus Inhibitors

scientific article published on 18 December 2018

Inhibiting the HIV integration process: past, present, and the future.

scientific article published on 25 September 2013

Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives

scientific article published in December 2017

Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties.

scientific article published in December 2017

In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51.

scientific article

Molecular Modeling of Azole Antifungal Agents Active againstCandida albicans. 1. A Comparative Molecular Field Analysis Study1

scientific article published on 01 March 1996

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

scientific article

Natural products as antifungal agents against clinically relevant pathogens

scientific article

New N,N-dimethylcarbamate inhibitors of acetylcholinesterase: design synthesis and biological evaluation

scientific article published on 3 September 2016

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

scientific article published on 7 May 2013

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.

scientific article

New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: discovery, characterization, and crystal structure in complex with the target

scientific article

New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation

scientific article published on 18 September 2017

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

scientific article published on 13 June 2011

Novel Benzazole Derivatives Endowed with Potent Antiheparanase Activity

scientific article published on 30 July 2018

Novel Symmetrical Benzazolyl Derivatives Endowed with Potent anti-Heparanase Activity

scientific article published on 29 November 2018

Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action

scientific article published on March 2006

Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities

scientific article published on 23 July 2008

Perturbing Effects of Chiral Stationary Phase on Enantiomerization Second-Order Rate Constants Determined by Enantioselective Dynamic High-Performance Liquid Chromatography: A Practical Tool to Quantify the Accessible Acid and Basic Catalytic Sites B

scientific article published on 01 May 2009

Pharmacophore Assessment Through 3-D QSAR: Evaluation of the Predictive Ability on New Derivatives by the Application on a Series of Antitubercular Agents

scientific article published on 17 May 2013

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors

scientific article published on 16 September 2013

Probing HIV-1 Integrase Inhibitor Binding Sites with Position-Specific Integrase-DNA Cross-Linking Assays

article

Pyrrolnitrin and related pyrroles endowed with antibacterial activities against Mycobacterium tuberculosis.

scientific article published on October 1998

Research on nitrogen containing heterocyclic compounds.XX. Synthesis of 8H-Imidazo[5,1-c]pyrrolo[1,2-a][1,4]benzodiazepine and its 6-derivatives

article published in 1993

Salmonella enterica serovar Typhimurium growth is inhibited by the concomitant binding of Zn(II) and a pyrrolyl-hydroxamate to ZnuA, the soluble component of the ZnuABC transporter

scientific article

Searching for new agents active against Candida albicans biofilm: A series of indole derivatives, design, synthesis and biological evaluation

scientific article published on 09 January 2019

Simple but highly effective three-dimensional chemical-feature-based pharmacophore model for diketo acid derivatives as hepatitis C virus RNA-dependent RNA polymerase inhibitors

scientific article published in October 2005

Structural Basis for Rational Design of Inhibitors Targeting Trypanosoma cruzi Sterol 14α-Demethylase: Two Regions of the Enzyme Molecule Potentiate Its Inhibition

scientific article

Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase.

scientific article published on 27 March 2017

Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain

scientific article published on 11 February 2015

Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: binding mode insights through magnesium complexation and site-directed mutagenesis studies

article

Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives

scientific article published on 26 January 2012

Synthesis and cerebral uptake of 1-(1-[(11)C]methyl-1H-pyrrol-2-yl)-2-phenyl-2-(1-pyrrolidinyl)ethanone, a novel tracer for positron emission tomography studies of monoamine oxidase type A.

scientific article

Synthesis, biological evaluation and structure-activity correlation study of a series of imidazol-based compounds as Candida albicans inhibitors

scientific article

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

Towards a new application of amaranth seed oil as an agent against Candida albicans

scientific article published on 04 December 2019

Will Integrase Inhibitors be Used as Microbicides? ⬇️

scientific article published on January 1, 2012

List of works by Roberto Di Santo

(Thiazol-2-yl)hydrazone derivatives from acetylpyridines as dual inhibitors of MAO and AChE: synthesis, biological evaluation and molecular modeling studies

1-Arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors

2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assays

2H-Pyrrolo[3,4-b] [1,5]benzothiazepine derivatives as potential inhibitors of HIV-1 reverse transcriptase

6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach

6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitro

6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays

A rational approach to predict and modulate stereolability of chiral alpha substituted ketones

Activity of caffeic acid derivatives against Candida albicans biofilm.

Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies

Antifungal agents. 11. N-substituted derivatives of 1-[(aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole: synthesis, anti-Candida activity, and QSAR studies

Antimycobacterial pyrroles: synthesis, anti-Mycobacterium tuberculosis activity and QSAR studies.

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 1).

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 2).

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

Biochemical characterization of a multi-drug resistant HIV-1 subtype AG reverse transcriptase: antagonism of AZT discrimination and excision pathways and sensitivity to RNase H inhibitors.

Cinnamoyl Compounds as Simple Molecules that Inhibit p300 Histone Acetyltransferase

Comparison of different methods for the extraction of cannabinoids from cannabis

Competing sigmatropic shift rearrangements in excited allyl radicals.

Convenient Route to 2H-Pyrrolo[3,4-b]quinolin-9(4H)-one Skeleton via TosMIC Reaction

Conversion of a racemic mixture of 8-chloro-2-(2,6-difluorophenylmethyl)-2,3-dihydro-3-methyl-1,2,5-benzothiadiazepin-4(5h)-one 1,1-dioxide into a single enantiomer via a chromatographic resolution/racemization method.

Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents

Design, synthesis and QSAR studies on N-aryl heteroarylisopropanolamines, a new class of non-peptidic HIV-1 protease inhibitors

Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors

Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitors

Design, synthesis, and structure-activity relationship of N-arylnaphthylamine derivatives as amyloid aggregation inhibitors

Design, synthesis, biological evaluation, and molecular modeling studies of TIBO-like cyclic sulfones as non-nucleoside HIV-1 reverse transcriptase inhibitors

Development of a human immunodeficiency virus vector-based, single-cycle assay for evaluation of anti-integrase compounds

Diaryl Disulfides as Novel Stabilizers of Tumor Suppressor Pdcd4

Diketo Acids Derivatives as Dual Inhibitors of Human Immunodeficiency Virus Type 1 Integrase and the Reverse Transcriptase RNase H Domain ⬇️

Diketo hexenoic acid derivatives are novel selective non-nucleoside inhibitors of mammalian terminal deoxynucleotidyl transferases, with potent cytotoxic effect against leukemic cells

Discovery and Pharmacological Profile of New 1H-Indazole-3-carboxamide and 2H-Pyrrolo[3,4-c]quinoline Derivatives as Selective Serotonin 4 Receptor Ligands

Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.

Discovery of in vitro antitubercular agents through in silico ligand-based approaches.

Effects of polyphenol compounds on influenza A virus replication and definition of their mechanism of action

Enantioselective liquid chromatography of C3-chiral 2,3-dihydro-1,2,5-benzothiadiazepin-4(5H)-one and thione 1,1-dioxides on polyacrylamide- and polysaccharide-based chiral stationary phases ⬇️

Evaluation of HIV-1 integrase inhibitors on human primary macrophages using a luciferase-based single-cycle phenotypic assay.

Evaluation of the Anti-<i>Histoplasma capsulatum</i> Activity of Indole and Nitrofuran Derivatives and Their Pharmacological Safety in Three-Dimensional Cell Cultures

Exploring the anti-biofilm activity of cinnamic acid derivatives in Candida albicans.

Geometrically and conformationally restrained cinnamoyl compounds as inhibitors of HIV-1 integrase: synthesis, biological evaluation, and molecular modeling.

HIV-1 RT-Associated RNase H Function Inhibitors: Recent Advances in Drug Development ⬇️

HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein

Human immunodeficiency virus type 1 (HIV-1) integration: a potential target for microbicides to prevent cell-free or cell-associated HIV-1 infection

Human terminal deoxynucleotidyl transferases as novel targets for anticancer chemotherapy

Hypoglycemic activity of curcumin synthetic analogues in alloxan-induced diabetic rats

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives

In Vitro Antiviral Activity of New Oxazoline Derivatives as Potent Poliovirus Inhibitors

Inhibiting the HIV integration process: past, present, and the future.

Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives

Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties.

In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51.

Molecular Modeling of Azole Antifungal Agents Active againstCandida albicans. 1. A Comparative Molecular Field Analysis Study1

N-Substituted Quinolinonyl Diketo Acid Derivatives as HIV Integrase Strand Transfer Inhibitors and Their Activity against RNase H Function of Reverse Transcriptase

Natural products as antifungal agents against clinically relevant pathogens

New N,N-dimethylcarbamate inhibitors of acetylcholinesterase: design synthesis and biological evaluation

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.

New nucleotide-competitive non-nucleoside inhibitors of terminal deoxynucleotidyl transferase: discovery, characterization, and crystal structure in complex with the target

New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

Novel Benzazole Derivatives Endowed with Potent Antiheparanase Activity

Novel Symmetrical Benzazolyl Derivatives Endowed with Potent anti-Heparanase Activity

Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action

Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities

Perturbing Effects of Chiral Stationary Phase on Enantiomerization Second-Order Rate Constants Determined by Enantioselective Dynamic High-Performance Liquid Chromatography: A Practical Tool to Quantify the Accessible Acid and Basic Catalytic Sites B

Pharmacophore Assessment Through 3-D QSAR: Evaluation of the Predictive Ability on New Derivatives by the Application on a Series of Antitubercular Agents

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors

Probing HIV-1 Integrase Inhibitor Binding Sites with Position-Specific Integrase-DNA Cross-Linking Assays

Pyrrolnitrin and related pyrroles endowed with antibacterial activities against Mycobacterium tuberculosis.

Research on nitrogen containing heterocyclic compounds.XX. Synthesis of 8H-Imidazo[5,1-c]pyrrolo[1,2-a][1,4]benzodiazepine and its 6-derivatives

Salmonella enterica serovar Typhimurium growth is inhibited by the concomitant binding of Zn(II) and a pyrrolyl-hydroxamate to ZnuA, the soluble component of the ZnuABC transporter

Searching for new agents active against Candida albicans biofilm: A series of indole derivatives, design, synthesis and biological evaluation

Simple but highly effective three-dimensional chemical-feature-based pharmacophore model for diketo acid derivatives as hepatitis C virus RNA-dependent RNA polymerase inhibitors

Structural Basis for Rational Design of Inhibitors Targeting Trypanosoma cruzi Sterol 14α-Demethylase: Two Regions of the Enzyme Molecule Potentiate Its Inhibition

Structure-Activity Relationships on Cinnamoyl Derivatives as Inhibitors of p300 Histone Acetyltransferase.

Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain

Structure-guided approach identifies a novel class of HIV-1 ribonuclease H inhibitors: binding mode insights through magnesium complexation and site-directed mutagenesis studies

Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives