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Article ; Online: In Vitro Combinatorial Activity of Direct Acting Antivirals and Monoclonal Antibodies against the Ancestral B.1 and BQ.1.1 SARS-CoV-2 Viral Variants.

Fiaschi, Lia / Biba, Camilla / Varasi, Ilenia / Bartolini, Niccolò / Paletti, Chiara / Giammarino, Federica / Saladini, Francesco / Zazzi, Maurizio / Vicenti, Ilaria

Viruses

2024 Volume 16, Issue 2

Abstract: Combination antiviral therapy may be helpful in the treatment of SARS-CoV-2 infection; however, no clinical trial data are available, and combined use of direct-acting antivirals (DAA) and monoclonal antibodies (mAb) has been reported only anecdotally. ... ...

Abstract	Combination antiviral therapy may be helpful in the treatment of SARS-CoV-2 infection; however, no clinical trial data are available, and combined use of direct-acting antivirals (DAA) and monoclonal antibodies (mAb) has been reported only anecdotally. To assess the cooperative effects of dual drug combinations in vitro, we used a VERO E6 cell-based in vitro system with the ancestral B.1 or the highly divergent BQ.1.1 virus to test pairwise combinations of the licensed DAA, including nirmatrelvir (NRM), remdesivir (RDV) and the active metabolite of molnupiravir (EIDD-1931) as well the combination of RDV with four licensed mAbs (sotrovimab, bebtelovimab, cilgavimab, tixagevimab; tested only with the susceptible B.1 virus). According to SynergyFinder 3.0 summary and weighted scores, all the combinations had an additive effect. Within DAA/DAA combinations, paired scores with the B.1 and BQ.1.1 variants were comparable. In the post hoc analysis weighting synergy by concentrations, several cases of highly synergistic scores were detected at specific drug concentrations, both for DAA/DAA and for RDV/mAb combinations. This was supported by in vitro confirmation experiments showing a more than a linear shift of a drug-effective concentration (IC
MeSH term(s)	Animals ; SARS-CoV-2/genetics ; Antiviral Agents/pharmacology ; COVID-19 ; Hepatitis C, Chronic ; Antibodies, Monoclonal/pharmacology ; Drug Combinations
Chemical Substances	Antiviral Agents ; Antibodies, Monoclonal ; Drug Combinations
Language	English
Publishing date	2024-01-23
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2516098-9
ISSN	1999-4915 ; 1999-4915
ISSN (online)	1999-4915
ISSN	1999-4915
DOI	10.3390/v16020168
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: HIV-1 Integrase Inhibition Activity by Spiroketals Derived from

Sanna, Cinzia / D'Abrosca, Brigida / Fiorentino, Antonio / Giammarino, Federica / Vicenti, Ilaria / Corona, Angela / Caredda, Alessia / Tramontano, Enzo / Esposito, Francesca

Pharmaceuticals (Basel, Switzerland)

2023 Volume 16, Issue 8

Abstract: In this work we investigated, for the first time, the effect ... ...

Abstract	In this work we investigated, for the first time, the effect of
Language	English
Publishing date	2023-08-08
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph16081118
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Article ; Online: Switching the three-component Biginelli-like reaction conditions for the regioselective synthesis of new 2-amino[1,2,4]triazolo[1,5-

Pacetti, Martina / Pismataro, Maria Chiara / Felicetti, Tommaso / Giammarino, Federica / Bonomini, Anna / Tiecco, Matteo / Bertagnin, Chiara / Barreca, Maria Letizia / Germani, Raimondo / Cecchetti, Violetta / Vicenti, Ilaria / Tabarrini, Oriana / Zazzi, Maurizio / Loregian, Arianna / Massari, Serena

Organic & biomolecular chemistry

2024 Volume 22, Issue 4, Page(s) 767–783

Abstract: Among the eight different triazolopyrimidine isomers existing in nature, 1,2,4-triazolo[1,5- ...

Abstract	Among the eight different triazolopyrimidine isomers existing in nature, 1,2,4-triazolo[1,5-
MeSH term(s)	Ionic Liquids ; Isomerism ; Pyrimidines/chemistry ; Stereoisomerism
Chemical Substances	Ionic Liquids ; Pyrimidines
Language	English
Publishing date	2024-01-24
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2097583-1
ISSN	1477-0539 ; 1477-0520
ISSN (online)	1477-0539
ISSN	1477-0520
DOI	10.1039/d3ob01861j
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Article ; Online: Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy.

Cesarini, Silvia / Vicenti, Ilaria / Poggialini, Federica / Filippi, Silvia / Mancin, Eleonora / Fiaschi, Lia / De Marchi, Elisa / Giammarino, Federica / Vagaggini, Chiara / Bizzarri, Bruno Mattia / Saladino, Raffaele / Dreassi, Elena / Zazzi, Maurizio / Botta, Lorenzo

Molecules (Basel, Switzerland)

2024 Volume 29, Issue 7

Abstract: The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the ... ...

Abstract	The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the modification of the chosen privileged framework and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized using a scaffold morphing approach consisting of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evaluated against lymphoma, hepatocarcinoma, and colon epithelial carcinoma cells, showing in five cases acceptable to good anticancer activity associated with low cytotoxicity on healthy fibroblasts. Finally, ADME in vitro studies were conducted on the best derivatives of the two series showing good passive permeability and resistance to metabolic degradation.
MeSH term(s)	Humans ; Antineoplastic Agents/pharmacology ; Antiviral Agents/pharmacology ; Azo Compounds ; Carcinoma, Hepatocellular ; Liver Neoplasms
Chemical Substances	Antineoplastic Agents ; Antiviral Agents ; Azo Compounds
Language	English
Publishing date	2024-03-24
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules29071452
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Zs.MO 81: Show issues

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Article ; Online: In vitro susceptibility of HIV-1 CRF02_AG to temsavir, the active compound of the attachment inhibitor fostemsavir.

Saladini, Francesco / Giannini, Alessia / Giammarino, Federica / Boccuto, Adele / Dragoni, Filippo / Vicenti, Ilaria / Zazzi, Maurizio

The Journal of antimicrobial chemotherapy

2021 Volume 76, Issue 12, Page(s) 3310–3312

MeSH term(s)	Anti-HIV Agents/pharmacology ; Anti-HIV Agents/therapeutic use ; HIV Infections/drug therapy ; HIV-1 ; Humans ; Organophosphates/therapeutic use ; Phylogeny ; Piperazines/therapeutic use
Chemical Substances	Anti-HIV Agents ; Organophosphates ; Piperazines ; fostemsavir (97IQ273H4L)
Language	English
Publishing date	2021-08-16
Publishing country	England
Document type	Letter ; Research Support, Non-U.S. Gov't
ZDB-ID	191709-2
ISSN	1460-2091 ; 0305-7453
ISSN (online)	1460-2091
ISSN	0305-7453
DOI	10.1093/jac/dkab309
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Zs.A 1197: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (1.OG) ab Jg. 2022: Lesesaal (EG)
Zs.MO 124: Show issues

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Article: Efficacy of Licensed Monoclonal Antibodies and Antiviral Agents against the SARS-CoV-2 Omicron Sublineages BA.1 and BA.2

Fiaschi, Lia / Dragoni, Filippo / Schiaroli, Elisabetta / Bergna, Annalisa / Rossetti, Barbara / Giammarino, Federica / Biba, Camilla / Gidari, Anna / Lai, Alessia / Nencioni, Cesira / Francisci, Daniela / Zazzi, Maurizio / Vicenti, Ilaria

Viruses. 2022 June 23, v. 14, no. 7

2022

Abstract: Newly emerging SARS-CoV-2 variants may escape monoclonal antibodies (mAbs) and antiviral drugs. By using live virus assays, we assessed the ex vivo inhibition of the B.1 wild-type (WT), delta and omicron BA.1 and BA.2 lineages by post-infusion sera from ... ...

Abstract	Newly emerging SARS-CoV-2 variants may escape monoclonal antibodies (mAbs) and antiviral drugs. By using live virus assays, we assessed the ex vivo inhibition of the B.1 wild-type (WT), delta and omicron BA.1 and BA.2 lineages by post-infusion sera from 40 individuals treated with bamlanivimab/etesevimab (BAM/ETE), casirivimab/imdevimab (CAS/IMD), and sotrovimab (SOT) as well as the activity of remdesivir, nirmatrelvir and molnupiravir. mAbs and drug activity were defined as the serum dilution (ID₅₀) and drug concentration (IC₅₀), respectively, showing 50% protection of virus-induced cytopathic effect. All pre-infusion sera were negative for SARS-CoV-2 neutralizing activity. BAM/ETE, CAS/IMD, and SOT showed activity against the WT (ID₅₀ 6295 (4355–8075) for BAM/ETE; 18,214 (16,248–21,365) for CAS/IMD; and 456 (265–592) for SOT) and the delta (14,780 (ID₅₀ 10,905–21,020) for BAM/ETE; 63,937 (47,211–79,971) for CAS/IMD; and 1103 (843–1334) for SOT). Notably, only SOT was active against BA.1 (ID₅₀ 200 (37–233)), whereas BA.2 was neutralized by CAS/IMD (ID₅₀ 174 (134–209) ID₅₀) and SOT (ID₅₀ 20 (9–31) ID₅₀), but not by BAM/ETE. No significant inter-variant IC₅₀ differences were observed for molnupiravir (1.5 ± 0.1/1.5 ± 0.7/1.0 ± 0.5/0.8 ± 0.01 μM for WT/delta/BA.1/BA.2, respectively), nirmatrelvir (0.05 ± 0.02/0.06 ± 0.01/0.04 ± 0.02/0.04 ± 0.01 μM) or remdesivir (0.08 ± 0.04/0.11 ± 0.08/0.05 ± 0.04/0.08 ± 0.01 μM). Continued evolution of SARS-CoV-2 requires updating the mAbs arsenal, although antivirals have so far remained unaffected.
Keywords	Severe acute respiratory syndrome coronavirus 2 ; antiviral agents ; blood serum ; cytopathogenicity ; evolution ; viruses
Language	English
Dates of publication	2022-0623
Publishing place	Multidisciplinary Digital Publishing Institute
Document type	Article
ZDB-ID	2516098-9
ISSN	1999-4915
ISSN	1999-4915
DOI	10.3390/v14071374
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Residual phenotypic susceptibility to doravirine in multidrug-resistant HIV-1 from subjects enrolled in the PRESTIGIO Registry.

Saladini, Francesco / Giammarino, Federica / Maggiolo, Franco / Ferrara, Micol / Cenderello, Giovanni / Celesia, Benedetto M / Martellotta, Ferdinando / Spagnuolo, Vincenzo / Corbelli, Giulio M / Gianotti, Nicola / Santoro, Maria M / Rusconi, Stefano / Zazzi, Maurizio / Castagna, Antonella

International journal of antimicrobial agents

2023 Volume 61, Issue 3, Page(s) 106737

Abstract: Objectives: Doravirine shows a rather distinct resistance profile within the nonnucleoside reverse transcriptase inhibitor (NNRTI) class. This study aimed to evaluate the phenotypic susceptibility to doravirine, rilpivirine and etravirine in a panel of ... ...

Abstract	Objectives: Doravirine shows a rather distinct resistance profile within the nonnucleoside reverse transcriptase inhibitor (NNRTI) class. This study aimed to evaluate the phenotypic susceptibility to doravirine, rilpivirine and etravirine in a panel of multidrug-resistant (MDR) HIV-1 isolates collected from people living with HIV (PLWH) enrolled in the PRESTIGIO Registry. Methods: Recombinant viruses expressing PLWH-derived protease, reverse transcriptase coding regions were generated from plasma samples at virological failure with documented resistance to protease inhibitors, nucleoside reverse transcriptase inhibitors, NNRTIs and integrase strand transfer inhibitors. In vitro susceptibility was assessed through a phenotypic assay measuring fold-change values with respect to the reference NL4-3 virus. Genotypic susceptibility was computed by the Stanford HIVdb algorithm 8.9-1. Results: Plasma samples were collected from 22 PLWH: 20 (91%) were male, median age 55 years (IQR 50-58), time since HIV-1 diagnosis 27 years (23-31) and time on antiretroviral treatment 23 years (22-26). Median doravirine, etravirine and rilpivirine fold-change values were 9.8 (2.9-40.4), 42.9 (3.1-100.0) and 100.0 (17.9-100.0), respectively. According to the fold-change cut-offs, full susceptibility was observed in five (23%), four (18%) and one (5%) cases with doravirine, etravirine and rilpivirine, respectively. Irrespective of the presence of specific doravirine mutations, higher numbers of NNRTI mutations correlated with higher fold-change values for doravirine. By comparing the distribution of fold-change values with the Stanford HIVdb predicted susceptibility, a significant correlation was detected for doravirine and rilpivirine but not etravirine. Conclusion: Despite extensive cross-resistance among NNRTIs, doravirine can be a valid option in a proportion of PLWH with MDR HIV-1. Doravirine activity appeared to be inferred with fair accuracy by the HIVdb algorithm.
MeSH term(s)	Humans ; Male ; Middle Aged ; Female ; HIV-1 ; Anti-HIV Agents/pharmacology ; Anti-HIV Agents/therapeutic use ; HIV Infections/drug therapy ; Reverse Transcriptase Inhibitors/pharmacology ; Reverse Transcriptase Inhibitors/therapeutic use ; Rilpivirine/therapeutic use ; Mutation ; Drug Resistance, Viral/genetics
Chemical Substances	Anti-HIV Agents ; doravirine (913P6LK81M) ; Reverse Transcriptase Inhibitors ; Rilpivirine (FI96A8X663) ; etravirine (0C50HW4FO1)
Language	English
Publishing date	2023-01-25
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1093977-5
ISSN	1872-7913 ; 0924-8579
ISSN (online)	1872-7913
ISSN	0924-8579
DOI	10.1016/j.ijantimicag.2023.106737
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Zs.A 3368: Show issues			Location: Je nach Verfügbarkeit (siehe Angabe bei Bestand) bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular Jg. 1995 - 2021: Lesesall (2.OG) ab Jg. 2022: Lesesaal (EG)
Zs.MO 500: Show issues

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Article ; Online: Nucleoside Derivatives of 2,6-Diaminopurine Antivirals: Base-Modified Nucleosides with Broad-Spectrum Antimicrobial Properties.

Grazia Martina, Maria / Giammarino, Federica / Vicenti, Ilaria / Groaz, Elisabetta / Rozenski, Jef / Incerti, Matteo / Sannio, Filomena / Docquier, Jean Denis / Zazzi, Maurizio / Radi, Marco

ChemMedChem

2023 Volume 18, Issue 16, Page(s) e202300200

Abstract: The plethora of viral outbreaks experienced in the last decade, together with the widespread distribution of many re-emerging and newly emerging viruses, emphasize the urgent need for novel broad-spectrum antivirals as tools for early intervention in ... ...

Abstract	The plethora of viral outbreaks experienced in the last decade, together with the widespread distribution of many re-emerging and newly emerging viruses, emphasize the urgent need for novel broad-spectrum antivirals as tools for early intervention in case of future epidemics. Non-natural nucleosides have been at the forefront for the treatment of infectious diseases for many years and still represent one of the most successful classes of antiviral molecules on the market. In the attempt to explore the biologically relevant chemical space of this class of antimicrobials, we describe herein the development of novel base-modified nucleosides by converting previously identified 2,6-diaminopurine antivirals into the corresponding D/L ribonucleosides, acyclic nucleosides and prodrug derivatives. A phenotypic screening against viruses belonging to different families (Flaviviridae, Coronaviridae, Retroviridae) and against a panel of Gram-positive and Gram-negative bacteria, allowed to identify a few interesting molecules with broad-spectrum antimicrobial activities.
MeSH term(s)	Humans ; Antiviral Agents/chemistry ; Nucleosides/chemistry ; Anti-Bacterial Agents/pharmacology ; Anti-Bacterial Agents/therapeutic use ; Gram-Negative Bacteria ; Gram-Positive Bacteria ; Viruses
Chemical Substances	Antiviral Agents ; Nucleosides ; 2,6-diaminopurine (49P95BAU4Z) ; Anti-Bacterial Agents
Language	English
Publishing date	2023-06-02
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.202300200
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Zs.A 6280: Show issues

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Article ; Online: Privileged Scaffold Decoration for the Identification of the First Trisubstituted Triazine with Anti-SARS-CoV-2 Activity.

Cesarini, Silvia / Vicenti, Ilaria / Poggialini, Federica / Secchi, Massimiliano / Giammarino, Federica / Varasi, Ilenia / Lodola, Camilla / Zazzi, Maurizio / Dreassi, Elena / Maga, Giovanni / Botta, Lorenzo / Saladino, Raffaele

Molecules (Basel, Switzerland)

2022 Volume 27, Issue 24

Abstract: Current therapy against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) are based on the use of ... ...

Abstract	Current therapy against severe acute respiratory syndrome coronavirus type 2 (SARS-CoV-2) are based on the use of Remdesivir
Language	English
Publishing date	2022-12-12
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules27248829
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Article ; Online: Efficacy of Licensed Monoclonal Antibodies and Antiviral Agents against the SARS-CoV-2 Omicron Sublineages BA.1 and BA.2.

Viruses

2022 Volume 14, Issue 7

Abstract	Newly emerging SARS-CoV-2 variants may escape monoclonal antibodies (mAbs) and antiviral drugs. By using live virus assays, we assessed the ex vivo inhibition of the B.1 wild-type (WT), delta and omicron BA.1 and BA.2 lineages by post-infusion sera from 40 individuals treated with bamlanivimab/etesevimab (BAM/ETE), casirivimab/imdevimab (CAS/IMD), and sotrovimab (SOT) as well as the activity of remdesivir, nirmatrelvir and molnupiravir. mAbs and drug activity were defined as the serum dilution (ID
MeSH term(s)	Antibodies, Monoclonal/pharmacology ; Antibodies, Monoclonal/therapeutic use ; Antibodies, Monoclonal, Humanized ; Antibodies, Neutralizing ; Antibodies, Viral ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19/drug therapy ; Humans ; Membrane Glycoproteins ; Neutralization Tests ; SARS-CoV-2 ; Spike Glycoprotein, Coronavirus ; Viral Envelope Proteins
Chemical Substances	Antibodies, Monoclonal ; Antibodies, Monoclonal, Humanized ; Antibodies, Neutralizing ; Antibodies, Viral ; Antiviral Agents ; Membrane Glycoproteins ; Spike Glycoprotein, Coronavirus ; Viral Envelope Proteins ; spike protein, SARS-CoV-2 ; sotrovimab (1MTK0BPN8V) ; imdevimab (2Z3DQD2JHM) ; bamlanivimab (45I6OFJ8QH) ; casirivimab (J0FI6WE1QN) ; etesevimab (N7Q9NLF11I)
Language	English
Publishing date	2022-06-23
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2516098-9
ISSN	1999-4915 ; 1999-4915
ISSN (online)	1999-4915
ISSN	1999-4915
DOI	10.3390/v14071374
Database	MEDical Literature Analysis and Retrieval System OnLINE

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