Pharmaceuticals,
Journal Year:
2024,
Volume and Issue:
17(12), P. 1664 - 1664
Published: Dec. 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.
Amino Acids,
Journal Year:
2024,
Volume and Issue:
56(1)
Published: March 20, 2024
Oxidative
stress
can
affect
the
protein,
lipids,
and
DNA
of
cells
thus,
play
a
crucial
role
in
several
pathophysiological
conditions.
It
has
already
been
established
that
oxidative
close
association
with
inflammation
via
nuclear
factor
erythroid
2-related
2
(NRF2)
signaling
pathway.
Amino
acids
are
notably
building
block
proteins
constitute
major
class
nitrogen-containing
natural
products
medicinal
importance.
They
exhibit
broad
spectrum
biological
activities,
including
ability
to
activate
NRF2,
transcription
regulates
endogenous
antioxidant
responses.
Moreover,
amino
may
act
as
synergistic
antioxidants
part
our
dietary
supplementations.
This
aroused
research
interest
NRF2-inducing
activity
acids.
Interestingly,
acids'
activation
NRF2-Kelch-like
ECH-associated
protein
1
(KEAP1)
pathway
exerts
therapeutic
effects
diseases.
Therefore,
present
review
will
discuss
relationship
between
different
NRF2-KEAP1
pinning
their
anti-inflammatory
properties.
We
also
discussed
formulations
applications
therapeutics.
broaden
prospect
myriad
stress-related
provide
an
insight
for
designing
developing
new
chemical
entities
NRF2
activators.
Archiv der Pharmazie,
Journal Year:
2024,
Volume and Issue:
357(9)
Published: May 31, 2024
Abstract
The
current
review
outlines
all
possible
recent
synthetic
platforms
to
quinoxaline
derivatives
and
the
potent
stimulated
apoptosis
mechanisms
targeted
by
anticancer
therapies.
currently
reported
results
disclosed
that
had
promising
potencies
against
a
wide
array
of
cancer
cell
lines,
better
than
reference
drugs,
through
target
inhibition.
This
summarizes
some
with
their
synthesis
strategies
potential
activities
various
molecular
targets.
Quinoxalines
can
be
considered
an
important
scaffold
for
inducers
in
cells
inhibiting
targets,
so
they
further
developed
as
target‐oriented
chemotherapeutics.
World Journal of Gastroenterology,
Journal Year:
2025,
Volume and Issue:
31(9)
Published: Feb. 18, 2025
Ulcerative
colitis
(UC),
a
chronic
and
challenging
condition,
necessitates
the
development
of
more
effective
treatments
owing
to
unsatisfactory
efficacy
side
effects
associated
with
current
medications.
Traditional
Chinese
medicine
(TCM),
known
for
its
multi-stage
multi-targeted
approach,
has
long
history
in
treating
gastrointestinal
diseases
offering
promising
alternative
UC
treatment.
Panax
ginseng
(P.
ginseng),
commonly
used
remedy
TCM,
exemplifies
this
potential,
although
specific
components
mechanisms
through
which
therapeutic
are
exerted
remain
be
fully
elucidated,
highlighting
need
further
research
unlock
full
potential
as
treatment
option.
To
investigate
key
constituents
biological
pathways
P.
exerts
on
UC.
Network
pharmacology
investigated
UC-alleviating
mechanism
ginseng,
including
"active
ingredient-target-disease"
network
analysis,
Gene
Ontology
Kyoto
Encyclopedia
Genes
Genomes
enrichment
analyses.
Panaxadiol
(PD;
active
ingredient
ginseng)
was
tested
mouse
model
3%
dextran
sulfate
sodium-induced
UC,
assessments
body
weight,
Disease
Activity
Index
scores,
colon
length.
Colitis
intestinal
barrier
integrity
were
analyzed
via
hematoxylin-eosin
Alcian
blue
periodic
acid-Schiff
staining,
immunohistochemistry,
real
time-quantitative
PCR,
western
blotting.
By
integrating
analyzing
targets
15
critical
hub
genes
discovered.
pathway
analysis
revealed
involved
linked
MAPK
PI3K-Akt
signaling.
Among
10
main
ingredients
identified
potentially
effective,
PD
most
abundant
validated
vivo
mitigate
weight
loss,
reduce
prevent
shortening.
also
reduced
inflammation
suppressed
expression
pro-inflammatory
cytokines
mediators.
In
addition,
increased
mucin
tight
junction
proteins.
Ultimately,
counteracted
sodium
by
inhibiting
phosphorylation
NF-кB
MAPK,
while
increasing
AMPK
NRF2
NQO1.
alleviates
aids
repair,
partly
modulation
MAPK/NF-кB
AMPK/NRF2/NQO1
pathways.
These
findings
suggest
new
methods
TCM.
The Journal of Organic Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 19, 2025
A
novel
[3+3]
cyclization
reaction
between
phenol
and
hydrazone
was
successfully
developed
under
electrochemically
driven
conditions.
This
provided
access
to
a
diverse
array
of
1,3,4-oxadiazinane
compounds
in
consistently
high
yields,
reaching
up
87%.
Notably,
the
exhibited
remarkable
tolerance
toward
broad
spectrum
both
substrates,
underscoring
its
versatility.
Moreover,
protocol
distinguished
itself
by
exceptional
atom
step
economy,
facilitating
efficient
construction
functionalized
1,3,4-oxadiazines.
The
synthetic
utility
this
approach
further
exemplified
scalability,
as
demonstrated
gram-scale
reactions,
substrate
scope.
