Pharmaceuticals,
Год журнала:
2024,
Номер
17(12), С. 1664 - 1664
Опубликована: Дек. 10, 2024
Background/Objectives:
The
alarming
rise
in
antibiotic
resistance
necessitates
the
discovery
of
novel
antimicrobial
agents.
This
study
aims
to
design,
synthesize,
and
evaluate
new
benzofuran–pyrazole-based
compounds
for
their
antimicrobial,
antioxidant,
anti-inflammatory
properties.
Methods:
New
benzofuran–pyrazole
hybrid
molecules
were
synthesized
using
Vilsmeier–Haach
reaction
other
chemical
processes.
structures
confirmed
through
micro-analytical
spectral
analyses.
Their
activities
assessed
against
various
bacterial
fungal
strains,
while
antioxidant
properties
evaluated
DPPH-free
radical
scavenging
HRBC
membrane
stabilization
assays,
respectively.
most
promising
further
tested
DNA
gyrase
B
inhibition.
Results:
Compounds
9,
10,
11b–d
exhibited
significant
broad-spectrum
activity
with
MIC
values
ranging
from
2.50
20
µg/mL.
4,
6,
11b,
11d
demonstrated
high
activity,
DPPH
percentages
between
84.16%
90.52%.
Most
showed
substantial
effects,
86.70%
99.25%.
Compound
9
notably
inhibited
E.
coli
an
IC50
9.80
µM,
comparable
ciprofloxacin.
Conclusions:
compounds,
particularly
compound
show
great
potential
as
agents
due
potent
These
findings
support
development
optimization
these
clinical
applications.
Science,
Год журнала:
2024,
Номер
386(6717), С. 99 - 105
Опубликована: Окт. 3, 2024
The
identity
of
a
heteroatom
within
an
aromatic
ring
influences
the
chemical
properties
that
heterocyclic
compound.
Systematically
evaluating
effect
single
atom,
however,
poses
synthetic
challenges,
primarily
as
result
thermodynamic
mismatches
in
atomic
exchange
processes.
We
present
photocatalytic
strategy
swaps
oxygen
atom
furan
with
nitrogen
group,
directly
converting
into
pyrrole
analog
intermolecular
reaction.
High
compatibility
was
observed
various
derivatives
and
nucleophiles
commonly
used
drug
discovery,
late-stage
functionalization
furnished
otherwise
difficult-to-access
pyrroles
from
naturally
occurring
furans
high
molecular
complexity.
Mechanistic
analysis
suggested
polarity
inversion
through
electron
transfer
initiates
redox-neutral
processes
at
room
temperature.
Abstract
Bacterial
infections,
particularly
those
associated
with
methicillin‐resistant
Staphylococcus
aureus
(MRSA)
and
vancomycin‐resistant
Enterococcus
(VRE),
threaten
public
health
economies,
rising
antibiotic
resistance
resulting
in
more
deaths
yearly.
In
this
study,
we
investigated
the
bacterial
inhibitory
activity
of
some
new
1,3,4‐oxadiazoles
prepared,
good
yields,
using
a
two‐step
tandem
protocol.
Therefore,
appropriate
N
‐benzoylhydrazones
were
prepared
first,
then,
without
isolation,
underwent
oxidative‐cyclization
presence
chloramine
trihydrate.
More
4‐acyloxyphenyl‐linked
by
pyridine‐mediated
acylation
2‐(4‐hydroxyphenyl)‐1,3,4‐oxadiazoles
acyl
chlorides.
Some
products
demonstrated
activity,
against
S.
faecalis
strains.
The
4‐(5‐(furan‐2‐yl)‐1,3,4‐oxadiazol‐2‐yl)phenyl
acetate
showed
comparable
antibacterial
to
ciprofloxacin,
MIC/MBC
values
up
3.6/7.2
µM
previous
Moreover,
it
different
MRSA
VRE
strains
when
compared
linezolid.
It
had
7.2/14.4
14.4/57.8
strains,
respectively.
Abstract
A
one‐pot,
electrochemical,
multicomponent
tandem
synthesis
of
trans
‐2,3‐dihydrobenzofuran
derivatives
is
reported.
Using
a
protic
solvent
in
an
undivided
cell
under
mild,
catalyst‐free
conditions,
the
obtained
substrate
yields
are
85%–93%.
This
electrochemical
approach
offers
attractive
alternative
to
conventional
synthetic
methods,
providing
environmentally
friendly
route
for
diastereoselective
synthesis.
Among
synthesized
compounds,
ten
were
selected
evaluation
DNA
cleavage
activity.
Compounds
4a
,
4b
4f
and
5c
demonstrated
notable
Additionally
vitro
anticancer
activity
studied
on
three
human
lines
includes
breast
cancer
line
(MCF‐7),
cervical
(HeLa),
leukemia
(K‐562),
among
five
evaluated
compounds
showed
lower
activity,
while
4e
4g,
5d
exhibited
enhanced
Notably,
compound
significant
across
all
lines.
Organic & Biomolecular Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
A
styrylogous
aldol
condensation
has
been
introduced,
constructing
2-styryl-benzofurans
in
high
yields.
The
method's
application
demonstrated
the
efficient
syntheses
of
biologically
active
aminostyryl-benzofurans
good
overall
Advanced Synthesis & Catalysis,
Год журнала:
2024,
Номер
366(9), С. 2101 - 2108
Опубликована: Март 5, 2024
Abstract
A
protocol
for
the
synthesis
of
trisubstituted
furans
via
phosphoric
acid‐catalyzed
regioselective
cascade
cyclization/amination
para
‐quinone
methides
(
p
‐QMs)
with
β
‐ketodinitriles
has
been
disclosed
first
time.
Various
kinds
‐QMs
and
can
effectively
produce
desired
polysubstituted
furan
derivatives
in
64–95%
yields,
demonstrating
high
atomic
economy
their
application
construction
heterocycles.
Preliminary
biological
activity
assay
suggests
that
these
have
potential
anticancer
activities.
