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Novel 2-Aryl-1H-Benzimidazole Derivatives and Their Aza-Analogues as Promising Anti-Poxvirus Agents
by
Lupinu, Ilenia
, Isola, Michela
, Virdis, Luca
, Manca, Valeria
, Murineddu, Gabriele
, Palmas, Vanessa
, Piras, Sandra
, Piras, Rebecca
, Sanna, Giuseppina
, Ibba, Roberta
, Sanna, Laura
, Serreli, Gabriele
, Locci, Laura
, Carta, Antonio
, Loddo, Roberta
in
Animals
/ Antiviral activity
/ Antiviral agents
/ Antiviral Agents - chemical synthesis
/ Antiviral Agents - chemistry
/ Antiviral Agents - pharmacology
/ Aza Compounds - chemistry
/ Aza Compounds - pharmacology
/ Benzimidazoles
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - chemistry
/ Benzimidazoles - pharmacology
/ Cell culture
/ Cell Line
/ Chlorocebus aethiops
/ Control
/ Cytotoxicity
/ Dosage and administration
/ Drug resistance
/ Epidemics
/ Genetic aspects
/ Health aspects
/ Heparan sulfate
/ Herpes viruses
/ Humans
/ Identification and classification
/ Infections
/ Monkeypox virus - drug effects
/ Mpox
/ MPXV
/ Orthopoxvirus
/ Orthopoxvirus - drug effects
/ Public health
/ Smallpox
/ Smallpox vaccine
/ TEER
/ Vaccination
/ Vaccines
/ Vaccinia
/ Vaccinia virus - drug effects
/ Viruses
2026
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Novel 2-Aryl-1H-Benzimidazole Derivatives and Their Aza-Analogues as Promising Anti-Poxvirus Agents
by
Lupinu, Ilenia
, Isola, Michela
, Virdis, Luca
, Manca, Valeria
, Murineddu, Gabriele
, Palmas, Vanessa
, Piras, Sandra
, Piras, Rebecca
, Sanna, Giuseppina
, Ibba, Roberta
, Sanna, Laura
, Serreli, Gabriele
, Locci, Laura
, Carta, Antonio
, Loddo, Roberta
in
Animals
/ Antiviral activity
/ Antiviral agents
/ Antiviral Agents - chemical synthesis
/ Antiviral Agents - chemistry
/ Antiviral Agents - pharmacology
/ Aza Compounds - chemistry
/ Aza Compounds - pharmacology
/ Benzimidazoles
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - chemistry
/ Benzimidazoles - pharmacology
/ Cell culture
/ Cell Line
/ Chlorocebus aethiops
/ Control
/ Cytotoxicity
/ Dosage and administration
/ Drug resistance
/ Epidemics
/ Genetic aspects
/ Health aspects
/ Heparan sulfate
/ Herpes viruses
/ Humans
/ Identification and classification
/ Infections
/ Monkeypox virus - drug effects
/ Mpox
/ MPXV
/ Orthopoxvirus
/ Orthopoxvirus - drug effects
/ Public health
/ Smallpox
/ Smallpox vaccine
/ TEER
/ Vaccination
/ Vaccines
/ Vaccinia
/ Vaccinia virus - drug effects
/ Viruses
2026
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Novel 2-Aryl-1H-Benzimidazole Derivatives and Their Aza-Analogues as Promising Anti-Poxvirus Agents
by
Lupinu, Ilenia
, Isola, Michela
, Virdis, Luca
, Manca, Valeria
, Murineddu, Gabriele
, Palmas, Vanessa
, Piras, Sandra
, Piras, Rebecca
, Sanna, Giuseppina
, Ibba, Roberta
, Sanna, Laura
, Serreli, Gabriele
, Locci, Laura
, Carta, Antonio
, Loddo, Roberta
in
Animals
/ Antiviral activity
/ Antiviral agents
/ Antiviral Agents - chemical synthesis
/ Antiviral Agents - chemistry
/ Antiviral Agents - pharmacology
/ Aza Compounds - chemistry
/ Aza Compounds - pharmacology
/ Benzimidazoles
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - chemistry
/ Benzimidazoles - pharmacology
/ Cell culture
/ Cell Line
/ Chlorocebus aethiops
/ Control
/ Cytotoxicity
/ Dosage and administration
/ Drug resistance
/ Epidemics
/ Genetic aspects
/ Health aspects
/ Heparan sulfate
/ Herpes viruses
/ Humans
/ Identification and classification
/ Infections
/ Monkeypox virus - drug effects
/ Mpox
/ MPXV
/ Orthopoxvirus
/ Orthopoxvirus - drug effects
/ Public health
/ Smallpox
/ Smallpox vaccine
/ TEER
/ Vaccination
/ Vaccines
/ Vaccinia
/ Vaccinia virus - drug effects
/ Viruses
2026
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Novel 2-Aryl-1H-Benzimidazole Derivatives and Their Aza-Analogues as Promising Anti-Poxvirus Agents
Journal Article
Novel 2-Aryl-1H-Benzimidazole Derivatives and Their Aza-Analogues as Promising Anti-Poxvirus Agents
2026
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Overview
Introduction: Despite the impressive progress carried out in the field of biomedical sciences in recent decades, the incidence of emerging and neglected lethal viral infections mainly belonging to the Coronaviridae, Filoviridae, Arenaviridae, Bunyaviridae, and Paramyxoviridae families has considerably impaired human health. The worldwide vaccination campaign at the end of the 1970s determined the eradication of smallpox. However, the growing number of cases of diseases linked to orthopoxvirus diseases, such as the recent epidemic of monkeypox zoonosis in various countries around the world, has increased the need for knowledge of these viral pathogens. To date, there is no specific treatement for Monkeypox virus (MPXV) infection. However, several antiviral drugs used to treat Smallpox and other viral infections could also be beneficial for Monkeypox disease. In this study we report the design and synthesis of new, variously substituted benzimidazole derivatives and the evaluation of their cytotoxicity and antiviral activity against representatives of the Orthopoxvirus genus, Vaccinia Virus (VV), closely related to variola virus and MPXV. Methods: A combination of cell-based assays and experimental techniques was used to investigate the cytotoxicity, antiviral activity, and mechanisms of action of the most interesting compound. Results: In our study, new, variously substituted benzimidazoles showed interesting EC50 values against vaccinia and MPXV and a cytotoxic profile in the high micromolar range. Conclusions: Our work shows that the new tested benzimidazole derivatives possess appealing activity and selectivity, accompanied by low cytotoxicity. These results set a valid foundation with which to identify potent and selective anti-Poxvirus agents.
Publisher
MDPI AG,Multidisciplinary Digital Publishing Institute (MDPI)
Subject
/ Antiviral Agents - chemical synthesis
/ Antiviral Agents - chemistry
/ Antiviral Agents - pharmacology
/ Aza Compounds - pharmacology
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - pharmacology
/ Control
/ Humans
/ Identification and classification
/ Monkeypox virus - drug effects
/ Mpox
/ MPXV
/ Orthopoxvirus - drug effects
/ Smallpox
/ TEER
/ Vaccines
/ Vaccinia
/ Vaccinia virus - drug effects
/ Viruses
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