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  1. Article ; Online: Special Issue "Advances in Antiviral Agents against SARS-CoV-2 and Its Variants".

    Esposito, Francesca / Cannalire, Rolando

    Viruses

    2023  Volume 15, Issue 9

    Abstract: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), with 770 million reported cases and around 7 million deaths, represents the worst pandemic in the last 100 years [ ... ]. ...

    Abstract Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), with 770 million reported cases and around 7 million deaths, represents the worst pandemic in the last 100 years [...].
    MeSH term(s) Humans ; SARS-CoV-2 ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19
    Chemical Substances Antiviral Agents
    Language English
    Publishing date 2023-09-10
    Publishing country Switzerland
    Document type Editorial
    ZDB-ID 2516098-9
    ISSN 1999-4915 ; 1999-4915
    ISSN (online) 1999-4915
    ISSN 1999-4915
    DOI 10.3390/v15091905
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: An overview on small molecules acting as broad-spectrum agents for yellow fever infection.

    Desantis, Jenny / Felicetti, Tommaso / Cannalire, Rolando

    Expert opinion on drug discovery

    2022  Volume 17, Issue 7, Page(s) 755–773

    Abstract: Introduction: Yellow fever virus (YFV) is a mosquito-borne flavivirus, endemic in 47 countries in Africa and South America, which causes febrile symptoms that can evolve in 15% of the patients to serious hemorrhagic conditions, liver injury, and ... ...

    Abstract Introduction: Yellow fever virus (YFV) is a mosquito-borne flavivirus, endemic in 47 countries in Africa and South America, which causes febrile symptoms that can evolve in 15% of the patients to serious hemorrhagic conditions, liver injury, and multiorgan failure. Although a highly effective vaccine (YF-17D vaccine) is available, to date, no antiviral drugs have been approved for the prevention and treatment of YFV infections.
    Areas covered: This review article focuses on the description of viral targets that have been considered within YFV and flavivirus drug discovery studies and on the most relevant candidates reported so far that elicit broad-spectrum inhibition against relevant strains and mutants of YFV.
    Expert opinion: Considering the growing interest on (re)emerging vector-borne viral infections, it is expected that flavivirus drug discovery will quickly deliver potential candidates for clinical evaluation. Due to similarity among flaviviral targets, several candidates identified against different flaviviruses have shown broad-spectrum activity, thus exhibiting anti-YFV activity, as well. In this regard, it would be desirable to routinely include the assessment of antiviral activity against different YFV strains. On the other hand, the development of host targeting agents are still at an initial stage and deserve further focused efforts.
    MeSH term(s) Animals ; Antiviral Agents/pharmacology ; Humans ; Yellow Fever/drug therapy ; Yellow Fever/prevention & control ; Yellow fever virus/physiology
    Chemical Substances Antiviral Agents
    Language English
    Publishing date 2022-06-24
    Publishing country England
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 2259618-5
    ISSN 1746-045X ; 1746-0441
    ISSN (online) 1746-045X
    ISSN 1746-0441
    DOI 10.1080/17460441.2022.2084529
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6388: Show issues Location:
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  3. Article ; Online: Broad-Spectrum Flavivirus Inhibitors: a Medicinal Chemistry Point of View.

    Felicetti, Tommaso / Manfroni, Giuseppe / Cecchetti, Violetta / Cannalire, Rolando

    ChemMedChem

    2020  Volume 15, Issue 24, Page(s) 2391–2419

    Abstract: Infections by flaviviruses, such as Dengue, West Nile, Yellow Fever and Zika viruses, represent a growing risk for global health. There are vaccines only for few flaviviruses while no effective treatments are available. Flaviviruses share epidemiological, ...

    Abstract Infections by flaviviruses, such as Dengue, West Nile, Yellow Fever and Zika viruses, represent a growing risk for global health. There are vaccines only for few flaviviruses while no effective treatments are available. Flaviviruses share epidemiological, structural, and ecologic features and often different viruses can co-infect the same host. Therefore, the identification of broad-spectrum inhibitors is highly desirable either for known flaviviruses or for viruses that likely will emerge in the future. Strategies targeting both virus and host factors have been pursued to identify broad-spectrum antiflaviviral agents. In this review, we describe the most promising and best characterized targets and their relative broad-spectrum inhibitors, identified by drug repurposing/libraries screenings and by focused medicinal chemistry campaigns. Finally, we discuss about future strategies to identify new broad-spectrum antiflavivirus agents.
    MeSH term(s) Animals ; Antiviral Agents/chemistry ; Antiviral Agents/pharmacokinetics ; Antiviral Agents/therapeutic use ; Cell Line, Tumor ; Chemistry, Pharmaceutical ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/therapeutic use ; Flavivirus/chemistry ; Flavivirus/drug effects ; Flavivirus/enzymology ; Flavivirus Infections/drug therapy ; Humans
    Chemical Substances Antiviral Agents ; Enzyme Inhibitors
    Language English
    Publishing date 2020-10-22
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2218496-X
    ISSN 1860-7187 ; 1860-7179
    ISSN (online) 1860-7187
    ISSN 1860-7179
    DOI 10.1002/cmdc.202000464
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6280: Show issues Location:
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  4. Article: Visible light photocatalysis in the late-stage functionalization of pharmaceutically relevant compounds

    Cannalire, Rolando / Pelliccia, Sveva / Sancineto, Luca / Novellino, Ettore / Tron, Gian Cesare / Giustiniano, Mariateresa

    Chemical Society reviews. 2021 Feb. 1, v. 50, no. 2

    2021  

    Abstract: The late stage functionalization (LSF) of complex biorelevant compounds is a powerful tool to speed up the identification of structure–activity relationships (SARs) and to optimize ADME profiles. To this end, visible-light photocatalysis offers unique ... ...

    Abstract The late stage functionalization (LSF) of complex biorelevant compounds is a powerful tool to speed up the identification of structure–activity relationships (SARs) and to optimize ADME profiles. To this end, visible-light photocatalysis offers unique opportunities to achieve smooth and clean functionalization of drugs by unlocking site-specific reactivities under generally mild reaction conditions. This review offers a critical assessment of current literature, pointing out the recent developments in the field while emphasizing the expected future progress and potential applications. Along with paragraphs discussing the visible-light photocatalytic synthetic protocols so far available for LSF of drugs and drug candidates, useful and readily accessible synoptic tables of such transformations, divided by functional groups, will be provided, thus enabling a useful, fast, and easy reference to them.
    Keywords drugs ; light ; literature ; moieties ; photocatalysis ; protocols ; society ; structure-activity relationships
    Language English
    Dates of publication 2021-0201
    Size p. 766-897.
    Publishing place The Royal Society of Chemistry
    Document type Article
    Note NAL-light
    ZDB-ID 1472875-8
    ISSN 1460-4744 ; 0306-0012
    ISSN (online) 1460-4744
    ISSN 0306-0012
    DOI 10.1039/d0cs00493f
    Database NAL-Catalogue (AGRICOLA)

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  5. Article: Visible-light photocatalytic metal-free multicomponent Ugi-like chemistry

    Russo, Camilla / Graziani, Giulia / Cannalire, Rolando / Tron, Gian Cesare / Giustiniano, Mariateresa

    Green chemistry. 2022 May 23, v. 24, no. 10

    2022  

    Abstract: The possibility of harnessing the photoactivity of isocyanides in the development of metal-free Ugi-like visible light photo-triggered multicomponent transformations has been reported herein. More in detail, Ugi-3CR, Ugi-Tetrazole-3CR, and Ugi–Joullié- ... ...

    Abstract The possibility of harnessing the photoactivity of isocyanides in the development of metal-free Ugi-like visible light photo-triggered multicomponent transformations has been reported herein. More in detail, Ugi-3CR, Ugi-Tetrazole-3CR, and Ugi–Joullié-3CR afforded imide peptidomimetic derivatives in good yields and with a wide substrate scope, involving the late-stage editing of complex bioactive scaffolds. Furthermore, a 2-step-one-pot sequence affording linear secondary imides, and a 3-step-one-pot protocol leading to densely functionalized bis-amide derivatives have also been developed to highlight the huge potential of these mild metal-free reaction conditions to afford complex and diverse compounds while being in accordance with the green chemistry principles.
    Keywords cyanides ; green chemistry ; imides ; light ; photocatalysis
    Language English
    Dates of publication 2022-0523
    Size p. 3993-4003.
    Publishing place The Royal Society of Chemistry
    Document type Article
    ZDB-ID 2006274-6
    ISSN 1463-9270 ; 1463-9262
    ISSN (online) 1463-9270
    ISSN 1463-9262
    DOI 10.1039/d2gc00855f
    Database NAL-Catalogue (AGRICOLA)

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  6. Article ; Online: Domino synthesis of 5-aminoimidazoles from Strecker multicomponent adducts via ytterbium-promoted isocyanide insertion/5-exo-dig cyclization.

    Cannalire, Rolando / Russo, Camilla / Luciano, Paolo / Cerra, Bruno / Gioiello, Antimo / Brunelli, Francesca / Tron, Gian Cesare / Giustiniano, Mariateresa

    Molecular diversity

    2022  Volume 27, Issue 1, Page(s) 511–515

    Abstract: A new Lewis acid promoted domino isocyanide insertion/5-exo-dig cyclization of readily available Strecker 3-component adducts to 4-substituted 5-aminoimidazole derivatives is herein reported. Despite their potential as relevant heterocyclic scaffolds in ... ...

    Abstract A new Lewis acid promoted domino isocyanide insertion/5-exo-dig cyclization of readily available Strecker 3-component adducts to 4-substituted 5-aminoimidazole derivatives is herein reported. Despite their potential as relevant heterocyclic scaffolds in medicinal chemistry programs, this class of compounds is still underrepresented, with current synthetic strategies poorly efficient in terms of timing and yields. To this end, we show how the exploitation of unconventional reactivities of isocyanides, promoted by ytterbium-triflate, could represent a key resource to enable a fast and easy access to such an unexplored area of the chemical space.
    MeSH term(s) Cyclization ; Cyanides/chemistry ; Ytterbium ; Imidazoles/chemistry
    Chemical Substances Cyanides ; 4-aminoimidazole (4919-03-3) ; Ytterbium (MNQ4O4WSI1) ; Imidazoles
    Language English
    Publishing date 2022-04-13
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1376507-3
    ISSN 1573-501X ; 1381-1991
    ISSN (online) 1573-501X
    ISSN 1381-1991
    DOI 10.1007/s11030-022-10418-4
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4946: Show issues Location:
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  7. Article ; Online: Visible-Light Photocatalytic Functionalization of Isocyanides for the Synthesis of Secondary Amides and Ketene Aminals.

    Cannalire, Rolando / Amato, Jussara / Summa, Vincenzo / Novellino, Ettore / Tron, Gian Cesare / Giustiniano, Mariateresa

    The Journal of organic chemistry

    2020  Volume 85, Issue 21, Page(s) 14077–14086

    Abstract: A new visible light-induced photocatalytic protocol enabling the formation of secondary amides from electron-poor organic bromides and isocyanides was developed. In addition, the in situ interception of ketenimine intermediates with nitrogen nucleophiles ...

    Abstract A new visible light-induced photocatalytic protocol enabling the formation of secondary amides from electron-poor organic bromides and isocyanides was developed. In addition, the in situ interception of ketenimine intermediates with nitrogen nucleophiles such as amines, hydrazines, and TMSN
    Language English
    Publishing date 2020-10-19
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.0c01946
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    Zs.A 4473: Show issues Location:
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  8. Article: Visible-Light Photocatalytic Functionalization of Isocyanides for the Synthesis of Secondary Amides and Ketene Aminals

    Cannalire, Rolando / Amato, Jussara / Summa, Vincenzo / Novellino, Ettore / Tron, Gian Cesare / Giustiniano, Mariateresa

    Journal of organic chemistry. 2020 Oct. 19, v. 85, no. 21

    2020  

    Abstract: A new visible light-induced photocatalytic protocol enabling the formation of secondary amides from electron-poor organic bromides and isocyanides was developed. In addition, the in situ interception of ketenimine intermediates with nitrogen nucleophiles ...

    Abstract A new visible light-induced photocatalytic protocol enabling the formation of secondary amides from electron-poor organic bromides and isocyanides was developed. In addition, the in situ interception of ketenimine intermediates with nitrogen nucleophiles such as amines, hydrazines, and TMSN₃ afforded, in a one-pot two-step procedure, valuable scaffolds such as ketene aminals, pyrazolones, and tetrazoles. Mechanistic evidence confirmed a radical pathway where isocyanides acted as radical geminal acceptors generating key imidoyl radical species.
    Keywords Lewis bases ; amides ; cyanides ; light ; nitrogen ; organic chemistry ; photocatalysis ; pyrazolones
    Language English
    Dates of publication 2020-1019
    Size p. 14077-14086.
    Publishing place American Chemical Society
    Document type Article
    ZDB-ID 123490-0
    ISSN 1520-6904 ; 0022-3263
    ISSN (online) 1520-6904
    ISSN 0022-3263
    DOI 10.1021/acs.joc.0c01946
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  9. Article ; Online: Photomicellar Catalyzed Synthesis of Amides from Isocyanides: Optimization, Scope, and NMR Studies of Photocatalyst/Surfactant Interactions.

    Cannalire, Rolando / Santoro, Federica / Russo, Camilla / Graziani, Giulia / Tron, Gian Cesare / Carotenuto, Alfonso / Brancaccio, Diego / Giustiniano, Mariateresa

    ACS organic & inorganic Au

    2021  Volume 2, Issue 1, Page(s) 66–74

    Abstract: The merging of micellar and photoredox catalysis represents a key issue to promote "in water" photochemical transformations. A photomicellar catalyzed synthesis of amides ... ...

    Abstract The merging of micellar and photoredox catalysis represents a key issue to promote "in water" photochemical transformations. A photomicellar catalyzed synthesis of amides from
    Language English
    Publishing date 2021-11-11
    Publishing country United States
    Document type Journal Article
    ISSN 2694-247X
    ISSN (online) 2694-247X
    DOI 10.1021/acsorginorgau.1c00028
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  10. Article ; Online: Visible light photocatalysis in the late-stage functionalization of pharmaceutically relevant compounds.

    Cannalire, Rolando / Pelliccia, Sveva / Sancineto, Luca / Novellino, Ettore / Tron, Gian Cesare / Giustiniano, Mariateresa

    Chemical Society reviews

    2020  Volume 50, Issue 2, Page(s) 766–897

    Abstract: The late stage functionalization (LSF) of complex biorelevant compounds is a powerful tool to speed up the identification of structure-activity relationships (SARs) and to optimize ADME profiles. To this end, visible-light photocatalysis offers unique ... ...

    Abstract The late stage functionalization (LSF) of complex biorelevant compounds is a powerful tool to speed up the identification of structure-activity relationships (SARs) and to optimize ADME profiles. To this end, visible-light photocatalysis offers unique opportunities to achieve smooth and clean functionalization of drugs by unlocking site-specific reactivities under generally mild reaction conditions. This review offers a critical assessment of current literature, pointing out the recent developments in the field while emphasizing the expected future progress and potential applications. Along with paragraphs discussing the visible-light photocatalytic synthetic protocols so far available for LSF of drugs and drug candidates, useful and readily accessible synoptic tables of such transformations, divided by functional groups, will be provided, thus enabling a useful, fast, and easy reference to them.
    MeSH term(s) Catalysis ; Drug Compounding ; Light ; Pharmaceutical Preparations/chemical synthesis ; Pharmaceutical Preparations/chemistry ; Photochemical Processes ; Structure-Activity Relationship
    Chemical Substances Pharmaceutical Preparations
    Language English
    Publishing date 2020-12-22
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1472875-8
    ISSN 1460-4744 ; 0306-0012
    ISSN (online) 1460-4744
    ISSN 0306-0012
    DOI 10.1039/d0cs00493f
    Database MEDical Literature Analysis and Retrieval System OnLINE

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