All Stories

  1. Tegaserod for the Treatment of Irritable Bowel Syndrome

    Article • Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry, October 2020, Bentham Science Publishers

    Dr Daniela De Vita, Roberto Di Santo

  2. Recent Advancement in the Search of Innovative Antiprotozoal Agents Targeting Trypanothione Metabolism

    Article • ChemMedChem, September 2020, Wiley

    Roberto Di Santo

  3. Comparison of different methods for the extraction of cannabinoids from cannabis

    Article • Natural Product Research, April 2019, Taylor & Francis

    Dr Daniela De Vita, Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, March 2019, Elsevier

    Roberto Di Santo

  5. 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 • MedChemComm, January 2018, Royal Society of Chemistry

    Roberto Di Santo

  6. New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation

    Article • European Journal of Medicinal Chemistry, December 2017, Elsevier

    Roberto Di Santo

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

    Article • ChemMedChem, April 2017, Wiley

    Roberto Di Santo

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

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, January 2017, Taylor & Francis

    Roberto Di Santo

  9. Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, January 2017, Taylor & Francis

    Roberto Di Santo

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

    Article • Bioorganic & Medicinal Chemistry Letters, December 2016, Elsevier

    Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, October 2016, Elsevier

    Roberto Di Santo

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

    Article • Antiviral Research, October 2016, Elsevier

    Roberto Di Santo

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

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, September 2016, Taylor & Francis

    Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, May 2016, Elsevier

    Roberto Di Santo

  15. Diaryl Disulfides as Novel Stabilizers of Tumor Suppressor Pdcd4

    Article • PLoS ONE, March 2016, PLOS

    Roberto Di Santo

  16. 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

    Article • Biochimica et Biophysica Acta (BBA) - General Subjects, March 2016, Elsevier

    Roberto Di Santo

  17. 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

    Article • Nucleic Acids Research, February 2016, Oxford University Press (OUP)

    Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, August 2015, Elsevier

    Roberto Di Santo

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

    Article • Journal of Medicinal Chemistry, May 2015, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, March 2015, Taylor & Francis

    Roberto Di Santo

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

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, February 2015, Taylor & Francis

    Professor Luciano Saso, Prof Kusal K. Das, Roberto Di Santo

  22. Structure–Activity Relationship of Pyrrolyl Diketo Acid Derivatives as Dual Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain

    Article • Journal of Medicinal Chemistry, February 2015, American Chemical Society (ACS)

    Roberto Di Santo

  23. The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

    Article • MedChemComm, January 2015, Royal Society of Chemistry

    Roberto Di Santo

  24. Identification of Highly Conserved Residues Involved in Inhibition of HIV-1 RNase H Function by Diketo Acid Derivatives

    Article • Antimicrobial Agents and Chemotherapy, August 2014, ASM Journals

    Enzo Tramontano, Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, August 2014, Elsevier

    Roberto Di Santo

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

    Article • Journal of Medicinal Chemistry, July 2014, American Chemical Society (ACS)

    Roberto Di Santo

  27. Correction to Inhibiting the HIV Integration Process: Past, Present, and the Future

    Article • Journal of Medicinal Chemistry, July 2014, American Chemical Society (ACS)

    Roberto Di Santo

  28. Basic Quinolinonyl Diketo Acid Derivatives as Inhibitors of HIV Integrase and their Activity against RNase H Function of Reverse Transcriptase

    Article • Journal of Medicinal Chemistry, April 2014, American Chemical Society (ACS)

    Roberto Di Santo

  29. Activity of caffeic acid derivatives against Candida albicans biofilm

    Article • Bioorganic & Medicinal Chemistry Letters, March 2014, Elsevier

    Roberto Di Santo

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

    Article • Journal of Enzyme Inhibition and Medicinal Chemistry, February 2014, Taylor & Francis

    Roberto Di Santo

  31. 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

    Article • Journal of Medicinal Chemistry, November 2013, American Chemical Society (ACS)

    Roberto Di Santo

  32. Inhibiting the HIV Integration Process: Past, Present, and the Future

    Article • Journal of Medicinal Chemistry, September 2013, American Chemical Society (ACS)

    Roberto Di Santo

  33. Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: A Suitable Scaffold for the Development of Noncamptothecin Topoisomerase I (Top1) Inhibitors

    Article • Journal of Medicinal Chemistry, September 2013, American Chemical Society (ACS)

    Roberto Di Santo

  34. New Nucleotide-Competitive Non-Nucleoside Inhibitors of Terminal Deoxynucleotidyl Transferase: Discovery, Characterization, and Crystal Structure in Complex with the Target

    Article • Journal of Medicinal Chemistry, September 2013, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Journal of Chemical Information and Modeling, May 2013, American Chemical Society (ACS)

    Roberto Di Santo

  36. New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

    Article • ACS Medicinal Chemistry Letters, May 2013, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Synthetic Communications, January 2013, Taylor & Francis

    Roberto Di Santo

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

    Article • Journal of Medicinal Chemistry, November 2012, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Biochimie, November 2012, Elsevier

    Roberto Di Santo

  40. Design, Synthesis, and Structure–Activity Relationship ofN-Arylnaphthylamine Derivatives as Amyloid Aggregation Inhibitors

    Article • Journal of Medicinal Chemistry, October 2012, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Bioorganic & Medicinal Chemistry, August 2012, Elsevier

    Roberto Di Santo

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

    Article • European Journal of Medicinal Chemistry, March 2012, Elsevier

    Roberto Di Santo

  43. Will Integrase Inhibitors be Used as Microbicides?

    Article • Current HIV Research, January 2012, Bentham Science Publishers

    Roberto Di Santo

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

    Article • Current Medicinal Chemistry, August 2011, Bentham Science Publishers

    Roberto Di Santo

  45. Novel 3,5-Bis(bromohydroxybenzylidene)piperidin-4-ones as Coactivator-Associated Arginine Methyltransferase 1 Inhibitors: Enzyme Selectivity and Cellular Activity

    Article • Journal of Medicinal Chemistry, July 2011, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Current Medicinal Chemistry, September 2010, Bentham Science Publishers

    Roberto Di Santo

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

    Article • Journal of Virological Methods, September 2010, Elsevier

    Roberto Di Santo

  48. Mass spectrometric characterization of tamoxifene metabolites in human urine utilizing different scan parameters on liquid chromatography/tandem mass spectrometry

    Article • Rapid Communications in Mass Spectrometry, February 2010, Wiley

    Roberto Di Santo

  49. Natural products as antifungal agents against clinically relevant pathogens

    Article • Natural Product Reports, January 2010, Royal Society of Chemistry

    Roberto Di Santo

  50. 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 Bon...

    Article • Analytical Chemistry, March 2009, American Chemical Society (ACS)

    Professor Marco Pierini, Roberto Di Santo

  51. Novel Quinolinonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, and Biological Activities

    Article • Journal of Medicinal Chemistry, August 2008, American Chemical Society (ACS)

    Roberto Di Santo

  52. A rational approach to predict and modulate stereolability of chiral α substituted ketones

    Article • Chirality, June 2008, Wiley

    Professor Marco Pierini, Roberto Di Santo

  53. Human Immunodeficiency Virus Type 1 (HIV-1) Integration: a Potential Target for Microbicides To Prevent Cell-Free or Cell-Associated HIV-1 Infection

    Article • Antimicrobial Agents and Chemotherapy, May 2008, ASM Journals

    Roberto Di Santo

  54. Competing sigmatropic shift rearrangements in excited allyl radicals

    Article • The Journal of Chemical Physics, April 2008, American Institute of Physics

    Roberto Di Santo

  55. Recent patents in antifungal agent discovery

    Article • Expert Opinion on Therapeutic Patents, March 2008, Informa Healthcare

    Roberto Di Santo

  56. Synthesis and Cerebral Uptake of 1-(1-[11C]Methyl-1H-pyrrol-2-yl)-2-phenyl-2-(1-pyrrolidinyl)ethanone, a Novel Tracer for Positron Emission Tomography Studies of Monoamine Oxidase Type A

    Article • Journal of Medicinal Chemistry, March 2008, American Chemical Society (ACS)

    Roberto Di Santo

  57. Cinnamoyl Compounds as Simple Molecules that Inhibit p300 Histone Acetyltransferase

    Article • Journal of Medicinal Chemistry, April 2007, American Chemical Society (ACS)

    Roberto Di Santo

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

    Article • Retrovirology, January 2007, Springer Science + Business Media

    Roberto Di Santo

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

    Article • Molecular Pharmacology, December 2006, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Roberto Di Santo

  60. Arylthiopyrrole (AThP) Derivatives as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: Synthesis, Structure–Activity Relationships, and Docking Studies (Part 1)

    Article • ChemMedChem, December 2006, Wiley

    Roberto Di Santo

  61. Arylthiopyrrole (AThP) Derivatives as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: Synthesis, Structure–Activity Relationships, and Docking Studies (Part 2)

    Article • ChemMedChem, December 2006, Wiley

    Roberto Di Santo

  62. Development of a Human Immunodeficiency Virus Vector-Based, Single-Cycle Assay for Evaluation of Anti-Integrase Compounds

    Article • Antimicrobial Agents and Chemotherapy, October 2006, ASM Journals

    Roberto Di Santo

  63. Human Terminal Deoxynucleotidyl Transferases as Novel Targets for Anticancer Chemotherapy

    Article • Current Medicinal Chemistry, August 2006, Bentham Science Publishers

    Roberto Di Santo

  64. Novel Bifunctional Quinolonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors:  Design, Synthesis, Biological Activities, and Mechanism of Action

    Article • Journal of Medicinal Chemistry, March 2006, American Chemical Society (ACS)

    Roberto Di Santo

  65. Design, Synthesis, Biological Evaluation, and Molecular Modeling Studies of TIBO-Like Cyclic Sulfones as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

    Article • ChemMedChem, January 2006, Wiley

    Roberto Di Santo

  66. Recent Developments in Antifungal Drug Discovery

    Article • January 2006, Elsevier

    Roberto Di Santo

  67. Simple but Highly Effective Three-Dimensional Chemical-Feature-Based Pharmacophore Model for Diketo Acid Derivatives as Hepatitis C Virus RNA-Dependent RNA Polymerase Inhibitors

    Article • Journal of Medicinal Chemistry, October 2005, American Chemical Society (ACS)

    Professor Sabrina Pricl, Roberto Di Santo

  68. Antifungal Agents. 11.N-Substituted Derivatives of 1-[(Aryl)(4-aryl-1H-pyrrol-3-yl)methyl]-1H-imidazole:  Synthesis, Anti-CandidaActivity, and QSAR Studies

    Article • Journal of Medicinal Chemistry, July 2005, American Chemical Society (ACS)

    Professor Letizia Angiolella, Roberto Di Santo

  69. Design, Synthesis, and Biological Activities of Pyrrolylethanoneamine Derivatives, a Novel Class of Monoamine Oxidases Inhibitors

    Article • Journal of Medicinal Chemistry, June 2005, American Chemical Society (ACS)

    Roberto Di Santo

  70. Diketo Hexenoic Acid Derivatives Are Novel Selective Non-Nucleoside Inhibitors of Mammalian Terminal Deoxynucleotidyl Transferases, with Potent Cytotoxic Effect against Leukemic Cells

    Article • Molecular Pharmacology, May 2005, American Society for Pharmacology & Experimental Therapeutics (ASPET)

    Roberto Di Santo

  71. 2H-Pyrrolo[3,4-b] [1,5]benzothiazepine derivatives as potential inhibitors of HIV-1 reverse transcriptase

    Article • Il Farmaco, May 2005, Elsevier

    Roberto Di Santo

  72. Design, synthesis and biological evaluation of heteroaryl diketohexenoic and diketobutanoic acids as HIV-1 integrase inhibitors endowed with antiretroviral activity

    Article • Il Farmaco, May 2005, Elsevier

    Roberto Di Santo

  73. 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

    Article • Antiviral Research, February 2005, Elsevier

    Roberto Di Santo

  74. 6-Aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assays

    Article • Bioorganic & Medicinal Chemistry Letters, April 2004, Elsevier

    Roberto Di Santo

  75. 2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone

    Article • Bioorganic & Medicinal Chemistry, January 2004, Elsevier

    Roberto Di Santo

  76. 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

    Article • Journal of Chromatography A, April 2003, Elsevier

    Roberto Di Santo

  77. 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

    Article • Chirality, January 2003, Wiley

    Roberto Di Santo

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

    Article • Bioorganic & Medicinal Chemistry, August 2002, Elsevier

    Roberto Di Santo

  79. Antifungal Agents. 10. New Derivatives of 1-[(Aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, Synthesis, Anti-CandidaActivity, and Quantitative Structure−Analysis Relationship Studies

    Article • Journal of Medicinal Chemistry, June 2002, American Chemical Society (ACS)

    Roberto Di Santo

  80. Analytical and semipreparative enantiomeric separation of azole antifungal agents by high-performance liquid chromatography on polysaccharide-based chiral stationary phases

    Article • Journal of Chromatography A, January 2002, Elsevier

    Roberto Di Santo

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

    Article • Bioorganic & Medicinal Chemistry, June 2000, Elsevier

    Roberto Di Santo

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

    Article • Bioorganic & Medicinal Chemistry Letters, October 1998, Elsevier

    Roberto Di Santo

  83. Geometrically and Conformationally Restrained Cinnamoyl Compounds as Inhibitors of HIV-1 Integrase:  Synthesis, Biological Evaluation, and Molecular Modeling

    Article • Journal of Medicinal Chemistry, September 1998, American Chemical Society (ACS)

    Roberto Di Santo

  84. 1-Arylsulfonyl-3-(α-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors

    Article • Bioorganic & Medicinal Chemistry Letters, July 1997, Elsevier

    Roberto Di Santo

  85. Antifungal estrogen-like imidazoles. Synthesis and antifungal activities of thienyl and 1H-pyrrolyl derivatives of 1-aryl-2-(1H-imidazol-1-yl)ethane

    Article • European Journal of Medicinal Chemistry, January 1997, Elsevier

    Roberto Di Santo

  86. Molecular Modeling of Azole Antifungal Agents Active against Candida albicans. 1. A Comparative Molecular Field Analysis Study

    Article • Journal of Medicinal Chemistry, March 1996, American Chemical Society (ACS)

    Roberto Di Santo

  87. Novel heterocyclic systems. Synthesis of 10H-Pyrrolo[1,2-b][1,2,5]-benzothiadiazocine 5,5-dioxide and related derivatives

    Article • Journal of Heterocyclic Chemistry, November 1995, Wiley

    Roberto Di Santo

  88. Pyrrolobenzodiazepines with antinociceptive activity: synthesis and pharmacological activities

    Article • European Journal of Medicinal Chemistry, January 1995, Elsevier

    Roberto Di Santo

  89. 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 • Journal of Heterocyclic Chemistry, May 1993, Wiley

    Roberto Di Santo

  90. Antifungal agents. 5. Chloro and amino derivatives of 1,2-diaryl-1-(1H-imidazol-1-yl)ethane with potent antifungal activities

    Article • European Journal of Medicinal Chemistry, January 1993, Elsevier

    Roberto Di Santo

  91. Antifungal agents. 1. Synthesis and antifungal activities of estrogen-like imidazole and triazole derivatives

    Article • European Journal of Medicinal Chemistry, August 1992, Elsevier

    Roberto Di Santo

  92. Pyrrylphenylethanones Related to Cathinone and Lefetamine: Synthesis and Pharmacological Activities

    Article • Archiv der Pharmazie, January 1992, Wiley

    Roberto Di Santo

  93. The Use Of Copper-(II) Bromide and N-Bromosuccinimide in the Bromination of 1-(1-Methyl-1H-pyrrol-2-yl)2-phenylethanone

    Article • Synthetic Communications, September 1989, Taylor & Francis

    Roberto Di Santo

  94. Heterocyclic systems.VIISynthesis of 1H-pyrazolo[3,4-e]indolizine derivatives

    Article • Journal of Heterocyclic Chemistry, July 1987, Wiley

    Roberto Di Santo