6 research outputs found
Base-mediated generation of ketenimines from ynamides: direct access to azetidinimines by an imino staudinger synthesis
Ynamides were used as precursors for the in situ generation of highly reactive ketenimines which could be trapped with imines in a [2+2] cycloaddition. This imino Staudinger synthesis led to a variety of imino-analogs of β-lactams, namely azetidinimines (20 examples), that could be further functionalized through a broad range of transformations
ChemInform Abstract: Epimerization and Kinetic Protonation as Factors Determining the Stereochemistry of the Michael Reaction.
Stereochemische Unterschiede bei der Michael Addition von Phenylessig-Estern und -Dialkylamiden an Methylcinnamat oder Methylcrotonat
Epimerisierung und kinetische Protonierung als Faktoren der Stereochemie der Michael-Reaktion
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