1 research outputs found
ボルツマンマシン ノ サイテキカ モンダイ エノ オウヨウ サイテキカ ノ スウリ ト ソノ オウヨウ
Influenza
is an infectious disease that represents an important
public health burden, with high impact on the global morbidity, mortality,
and economy. The poor protection and the need of annual updating of
the anti-influenza vaccine, added to the rapid emergence of viral
strains resistant to current therapy make the need for antiviral drugs
with novel mechanisms of action compelling. In this regard, the viral
RNA polymerase is an attractive target that allows the design of selective
compounds with reduced risk of resistance. In previous studies we
showed that the inhibition of the polymerase acidic protein-basic
protein 1 (PA–PB1) interaction is a promising strategy for
the development of anti-influenza agents. Starting from the previously
identified 3-cyano-4,6-diphenyl-pyridines, we chemically modified
this scaffold and explored its structure–activity relationships.
Noncytotoxic compounds with both the ability of disrupting the PA–PB1
interaction and antiviral activity were identified, and their mechanism
of target binding was clarified with molecular modeling simulations