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  1. Article ; Online: Viral Envelope Membrane: A Special Entry Pathway and a Promising Drug Target.

    Palombi, Nastasja / Brai, Annalaura / Gerace, Martina / Di Maria, Salvatore / Orofino, Francesco / Corelli, Federico

    Current medicinal chemistry

    2021  Volume 28, Issue 34, Page(s) 6957–6976

    Abstract: Enveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 ... ...

    Abstract Enveloped viruses belong to a large class of pathogens responsible for multiple serious diseases. Their spread into new territories has been the cause of major epidemics throughout human history, including the Spanish flu in 1918 and the latest COVID-19 pandemic. Thanks to their outer membrane, consisting essentially of host lipids, enveloped viruses are more resistant to enzymes and are also less susceptible to host immune defenses than their naked counterparts. Therefore, the development of effective approaches to combat enveloped virus infections represents a major challenge for antiviral therapy in the current century. This review focuses on the characteristics of enveloped viruses, their importance in the entry phase, drugs targeting envelope membrane- mediated entry, and those specifically designed to target the envelope. The broad- -spectrum antiviral activity of these compounds can be attributed to their ability to affect the envelope, an essential structural feature common to several viruses. This makes this class of compounds agents of great interest when no specific drugs or vaccines are available to block viral infections.
    MeSH term(s) Antiviral Agents/pharmacology ; COVID-19 ; Humans ; Influenza Pandemic, 1918-1919 ; Pandemics ; Pharmaceutical Preparations ; SARS-CoV-2 ; Viral Envelope ; Virus Internalization
    Chemical Substances Antiviral Agents ; Pharmaceutical Preparations
    Language English
    Publishing date 2021-02-18
    Publishing country United Arab Emirates
    Document type Journal Article ; Review
    ZDB-ID 1319315-6
    ISSN 1875-533X ; 0929-8673
    ISSN (online) 1875-533X
    ISSN 0929-8673
    DOI 10.2174/0929867328666210218182203
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.

    Mugnaini, Claudia / Rabbito, Alessandro / Brizzi, Antonella / Palombi, Nastasja / Petrosino, Stefania / Verde, Roberta / Di Marzo, Vincenzo / Ligresti, Alessia / Corelli, Federico

    European journal of medicinal chemistry

    2018  Volume 161, Page(s) 239–251

    Abstract: A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position ... ...

    Abstract A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ring possess high CB2R affinity at low nanomolar concentration, good receptor selectivity, and agonistic functional activity. The full agonist 8g, showing the best balance between receptor affinity and selectivity, was tested in vitro in an experimental model of allergic contact dermatitis and proved to be able to block the release of MCP-2 in HaCaT cells at 10 μM concentration.
    MeSH term(s) Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Cell Line ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; HEK293 Cells ; Humans ; Immunosuppressive Agents/chemical synthesis ; Immunosuppressive Agents/chemistry ; Immunosuppressive Agents/pharmacology ; Inflammation/drug therapy ; Inflammation/pathology ; Keratinocytes/drug effects ; Molecular Structure ; Receptor, Cannabinoid, CB2/agonists ; Skin Diseases/drug therapy ; Skin Diseases/pathology ; Structure-Activity Relationship ; Thiophenes/chemical synthesis ; Thiophenes/chemistry ; Thiophenes/pharmacology
    Chemical Substances Anti-Inflammatory Agents, Non-Steroidal ; Immunosuppressive Agents ; Receptor, Cannabinoid, CB2 ; Thiophenes
    Language English
    Publishing date 2018-10-13
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2018.09.070
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein.

    Mori, Mattia / Dasso Lang, Maria Chiara / Saladini, Francesco / Palombi, Nastasja / Kovalenko, Lesia / De Forni, Davide / Poddesu, Barbara / Friggeri, Laura / Giannini, Alessia / Malancona, Savina / Summa, Vincenzo / Zazzi, Maurizio / Mely, Yves / Botta, Maurizio

    ACS medicinal chemistry letters

    2018  Volume 10, Issue 4, Page(s) 463–468

    Abstract: Small molecule inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and ...

    Abstract Small molecule inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and tested
    Language English
    Publishing date 2018-12-07
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.8b00506
    Database MEDical Literature Analysis and Retrieval System OnLINE

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