Roberto Di Santo

Pubblicazioni

Titolo Pubblicato in Anno
Effect of Heparanase inhibitor on Tissue Factor overexpression in platelets and endothelial cells induced by anti-β2-GPI antibodies JOURNAL OF THROMBOSIS AND HAEMOSTASIS 2021
Quinolinonyl non-diketo acid derivatives as Inhibitors of HIV-1 ribonuclease H and polymerase functions of reverse transcriptase JOURNAL OF MEDICINAL CHEMISTRY 2021
Recent advances in recovery of lycopene from tomato waste. A potent antioxidant with endless benefits MOLECULES 2021
Toxicological aspects of cannabinoid, pesticide and metal levels detected in light Cannabis inflorescences grown in Italy FOOD AND CHEMICAL TOXICOLOGY 2021
Small-molecule inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H function. Challenges and recent developments CURRENT MEDICINAL CHEMISTRY 2021
New pyrimidine and pyridine derivatives as multitarget cholinesterase inhibitors. Design, synthesis, and in vitro and in cellulo evaluation ACS CHEMICAL NEUROSCIENCE 2021
Salmonella typhimurium and pseudomonas aeruginosa respond differently to the fe chelator deferiprone and to some novel deferiprone derivatives INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES 2021
Discovery of a pyrimidine compound endowed with antitumor activity INVESTIGATIONAL NEW DRUGS 2020
New deferiprone derivatives as multi-functional cholinesterase inhibitors. Design, synthesis and in vitro evaluation EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 2020
Pyrrolyl pyrazoles as non-diketo acid inhibitors of the HIV-1 ribonuclease H function of reverse transcriptase ACS MEDICINAL CHEMISTRY LETTERS 2020
Discovery of dihydroxyindole-2-carboxylic acid derivatives as dual allosteric HIV-1 integrase and reverse transcriptase associated ribonuclease H inhibitors ANTIVIRAL RESEARCH 2020
Recent Advancement in the Search of Innovative Antiprotozoal Agents Targeting Trypanothione Metabolism CHEMMEDCHEM 2020
In vitro antiviral activity of new oxazoline derivatives as potent poliovirus inhibitors JOURNAL OF MEDICINAL CHEMISTRY 2019
Searching for new agents active against candida albicans biofilm: a series of indole derivatives, design, synthesis and biological evaluation EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 2019
Design, synthesis, and biological evaluation of new 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole derivatives as antiprotozoal agents JOURNAL OF MEDICINAL CHEMISTRY 2019
Comparison of different methods for the extraction of cannabinoids from cannabis NATURAL PRODUCT RESEARCH 2019
Inhibition of Polycomb Repressive Complex2 activity reduces trimethylation of H3K27 and affects development in Arabidopsis seedlings BMC PLANT BIOLOGY 2019
Structure-guided approach to identify a novel class of anti-leishmaniasis diaryl sulfide compounds targeting the trypanothione metabolism AMINO ACIDS 2019
Towards a new application of amaranth seed oil as an agent against Candida albicans NATURAL PRODUCT RESEARCH 2019
Tegaserod for the treatment of Irritable Bowel syndrome ANTI-INFLAMMATORY & ANTI-ALLERGY AGENTS IN MEDICINAL CHEMISTRY 2019

ERC

  • PE5_18

KET

  • Life-science technologies & biotechnologies

Interessi di ricerca

Drug Design.

Antimicrobial agents active agains virues  such as HIV, SARSCoV, HCV, CHIKV,

Antibacterial agents based on quinolone scaffold. Metallo-beta-lactamase inhibitors.

Antiprotozoals

Antifungals

Antimycobacterals

Antitumor agenst with specific mechanism of action: Kinase Inhibitors. Inhibitors of tubulin polimerization. Antitumoral agents found by phenotypic approach.

Natural substances: plant extracts for medicinal and nutraceutical applications.

My laboratory is involved in design and synthesis of compounds active against various microbial agents.
We use the most modern synthetic approaches like microwave heating flow chemistry, parallel synthesis,
as well as the classic batch approach to synthesize the designed compounds.
Big expertise in the design and synthesis of compounds active against a number of targets of HIV, HCV, fungi, protozoa and bacteria. Decennial experience in this field led to the discovery of compounds with potent activity against integrase, in particular on the strand transfer step of integration process. The studied started in the last part of 90s, with the discovery of the first group synthetic polyhydroxy aromatic derivatives that inhibited IN activities.  Later, new ADK compounds characterized by a pyrrole and or quinoline ring that were very potent IN inhibitors active in cell-based assays, have been designed and synthesized. Several molecular tools have been designed that contributed to understand the mechanism of action of HIV Integrase. Expertise also in other fields of the medicinal chemistry: antifungal and antiprotozoal agents, compounds active against HCV polymerase, anti-TBC, as well as chemotherapeutic agents useful against liquid and solid tumors.

Several  interaction with Companies, to develop antimalarial agents, ligands of 5-HT receptors, and compounds active against the aggregation of beta-amyloid fibrils:

Project “beta-amiloid” (Sigma-Tau);
“Malaria - Artekin” (Sigma-Tau);
Project “New ligands of 5-HT4 receptors” (ACRAF).
Project “Triamcinolone” (AlfaSigma)
Project Heparanase Inhibitors (AlfaSigma)
Project Combiotic specifications (Pfizer)
Project MBL inhibitors (Microbo)

 

Keywords

drug design and synthesis.
antiviral agents
antibacterial agents
antifungal agents
Antiprotozoal Agents
antimycobacterial agents
antitumor agents
tyrosine kinase inhibitors
tubulin inhibitors

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