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2020 ; 25
(7
): ä Nephropedia Template TP
gab.com Text
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Synthesis and Biological Evaluation of Novel (thio)semicarbazone-Based
Benzimidazoles as Antiviral Agents against Human Respiratory Viruses
#MMPMID32218301
Francesconi V
; Cichero E
; Schenone S
; Naesens L
; Tonelli M
Molecules
2020[Mar]; 25
(7
): ä PMID32218301
show ga
Respiratory RNA viruses are responsible for recurrent acute respiratory illnesses
that still represent a major medical need. Previously we developed a large
variety of benzimidazole derivatives able to inhibit these viruses. Herein, two
series of (thio)semicarbazone- and hydrazone-based benzimidazoles have been
explored, by derivatizing 5-acetyl benzimidazoles previously reported by us,
thereby evaluating the influence of the modification on the antiviral activity.
Compounds 6, 8, 16 and 17, bearing the 5-(thio)semicarbazone and 5-hydrazone
functionalities in combination with the 2-benzyl ring on the benzimidazole core
structure, acted as dual inhibitors of influenza A virus and human coronavirus.
For respiratory syncytial virus (RSV), activity is limited to the
5-thiosemicarbazone (25) and 5-hydrazone (22) compounds carrying the
2-[(benzotriazol-1/2-yl)methyl]benzimidazole scaffold. These molecules proved to
be the most effective antiviral agents, able to reach the potency profile of the
licensed drug ribavirin. The molecular docking analysis explained the SAR of
these compounds around their binding mode to the target RSV F protein, revealing
the key contacts for further assessment. The herein-investigated
benzimidazole-based derivatives may represent valuable hit compounds, deserving
subsequent structural improvements towards more efficient antiviral agents for
the treatment of pathologies caused by these human respiratory viruses.
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