Abstract
In
recent
years,
selenocompounds
have
gained
increasing
attention
as
potential
anticancer
and
antibacterial
agents.
Several
selenoderivatives
been
confirmed
to
act
MDR
efflux
pump
inhibitors,
based
on
their
in
vitro
results
against
the
bacterial
AcrAB‐TolC
system
cancer
P‐glycoprotein.
Efflux
pumps
can
contribute
directly
or
indirectly
virulence
of
bacteria,
they
reduce
intracellular
concentration
substances
by
expelling
them
out
cell.
The
present
work
aims
study
inhibiting
properties
four
families
selenoesters,
namely
aspirin‐selenoesters,
phenone‐selenoesters,
hydroxy‐selenoesters,
benzyl‐selenoesters.
real‐time
ethidium
bromide
accumulation
assay
that
these
derivatives
inhibited
systems
methicillin‐resistant
Staphylococcus
aureus
(MRSA)
without
exerting
any
effect.
relative
expression
gene
NorA
transporter
was
also
monitored
presence
most
potent
reference
S.
,
finding
could
change
tested
gene.
Regarding
anti‐biofilm
activity,
benzyl‐selenoesters,
hydroxy‐selenoesters
efficiently
inhibit
biofilm
production
MRSA
strain.
It
be
concluded
thus
reducing
biofilm‐producing
bacteria.
The Journal of Organic Chemistry,
Год журнала:
2024,
Номер
89(9), С. 6520 - 6526
Опубликована: Апрель 11, 2024
An
available
and
simple
electromediated
cyclization
method
for
3-amino-substituted
pyrazoles
by
using
α,β-alkynic
hydrazone
secondary
amine
is
described.
The
strategy
utilizes
KI
as
an
electrolyte
in
undivided
cell
with
a
constant
current,
generating
the
desired
products
moderate-to-good
yield.
features
selective
amination
at
3-position
of
pyrazole
skeleton.
results
indicate
that
hydrazones
functionalized
aromatic
groups
amines
electron-rich
were
better
tolerated
this
transformation.
Advanced Synthesis & Catalysis,
Год журнала:
2024,
Номер
unknown
Опубликована: Окт. 19, 2024
Abstract
Electrosynthesis
of
selenylated‐oxazolone
derivatives
via
cascade
selenylation/cyclization
ynamides
was
disclosed.
A
series
diaryl
diselenides,
dialkyl
and
heteroaryl‐substituted
tolerated
in
this
protocol
delivered
4‐selenyloxazolones
28–83%
yields.
The
scale‐up
reaction
the
oxidation
performed
to
showcase
practicability
method.
Furthermore,
mechanistic
experiments
indicated
that
a
cationic
pathway
instead
radical
probably
involved.
Angewandte Chemie,
Год журнала:
2023,
Номер
135(45)
Опубликована: Сен. 12, 2023
Abstract
Despite
widespread
use
of
the
deuterium
isotope
effect,
selective
labeling
chemical
molecules
remains
a
major
challenge.
Herein,
facile
and
general
electrochemically
driven,
organic
mediator
enabled
deuteration
styrenes
with
oxide
(D
2
O)
as
economical
source
was
reported.
Importantly,
this
transformation
could
be
suitable
for
various
electron
rich
mediated
by
triphenylphosphine
(TPP).
The
reaction
proceeded
under
mild
conditions
without
transition‐metal
catalysts,
affording
desired
products
in
good
yields
excellent
D‐incorporation
(D‐inc,
up
to
>99
%).
Mechanistic
investigations
means
experiments
cyclic
voltammetry
tests
provided
sufficient
support
transformation.
Notably,
method
proved
powerful
tool
late‐stage
biorelevant
compounds.
Chemical Communications,
Год журнала:
2024,
Номер
60(65), С. 8573 - 8576
Опубликована: Янв. 1, 2024
An
electrochemical
protocol
for
the
synthesis
of
sulfursulfoxonium
ylides
and
1,3-dithioketals
by
reacting
sulfoxonium
with
disulfides
has
been
developed
under
simple
mild
conditions.
By
changing
solubility
raw
materials
dielectric
parameters
electrolyte,
sulfurization
enabled
a
selective
dehydrogenation
C-S
construction
1,3-dithioketals.
The
transformation
is
an
ideal
approach
to
prepare
organosulfur
reagents
broad
functional
group
tolerance
as
well
high
selectivity,
which
leads
vicinal
difunctionalized
compounds.
Advanced Synthesis & Catalysis,
Год журнала:
2023,
Номер
366(2), С. 188 - 193
Опубликована: Дек. 1, 2023
Abstract
A
direct
electrosynthesis
of
cyclic
isoureas
from
N
‐allyl
ureas
and
diselenides
has
been
described.
This
protocol
proceeds
without
any
additional
catalyst
oxidant,
at
room
temperature
under
air,
providing
the
desired
products
in
71–91%
yield.
In
addition,
synthesis
containing
five
to
seven‐membered
rings
also
achieved
by
employment
this
strategy.
On
basis
mechanism
experiments
previous
research
works,
a
probable
is
proposed.
Abstract
In
recent
years,
selenocompounds
have
gained
increasing
attention
as
potential
anticancer
and
antibacterial
agents.
Several
selenoderivatives
been
confirmed
to
act
MDR
efflux
pump
inhibitors,
based
on
their
in
vitro
results
against
the
bacterial
AcrAB‐TolC
system
cancer
P‐glycoprotein.
Efflux
pumps
can
contribute
directly
or
indirectly
virulence
of
bacteria,
they
reduce
intracellular
concentration
substances
by
expelling
them
out
cell.
The
present
work
aims
study
inhibiting
properties
four
families
selenoesters,
namely
aspirin‐selenoesters,
phenone‐selenoesters,
hydroxy‐selenoesters,
benzyl‐selenoesters.
real‐time
ethidium
bromide
accumulation
assay
that
these
derivatives
inhibited
systems
methicillin‐resistant
Staphylococcus
aureus
(MRSA)
without
exerting
any
effect.
relative
expression
gene
NorA
transporter
was
also
monitored
presence
most
potent
reference
S.
,
finding
could
change
tested
gene.
Regarding
anti‐biofilm
activity,
benzyl‐selenoesters,
hydroxy‐selenoesters
efficiently
inhibit
biofilm
production
MRSA
strain.
It
be
concluded
thus
reducing
biofilm‐producing
bacteria.
