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J Biol Inorg Chem ; 27(4-5): 421-429, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35332377

RESUMO

In this work, a synthetic approach to prepare an example of new class of the derivatives of the closo-decaborate anion with amino acids detached from the boron cluster by pendant group has been proposed and implemented. Compound Na2[B10H9-O(CH2)4C(O)-His-OMe] was isolated and characterized. This compound has an inorganic hydrophobic core which is the 10-vertex boron cage and the -O(CH2)4C(O)-His-OMe organic substituent. It has been shown to possess strong antiviral activity in vitro against modern strains of A/H1N1 virus at 10 and 5 µg/mL. The compound has been found to be non-cytotoxic up to 160 µg/mL. At the same time, the compound has been found to be inactive against SARS-CoV-2, indicating specific activity against RNA virus replication. Molecular docking of the target derivative of the closo-decaborate anion with a model of the transmembrane region of the M2 protein has been performed and the mechanism of its antiviral action is discussed.


Assuntos
COVID-19 , Vírus da Influenza A Subtipo H1N1 , Aminoácidos , Ânions , Antivirais/farmacologia , Boro/química , Ésteres/farmacologia , Humanos , Simulação de Acoplamento Molecular , RNA , SARS-CoV-2 , Replicação Viral
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