Thirteen
novel
Schiff
base
benzopyranone
derivatives(TEMC-1~TEMC-13)
were
synthesized
by
nucleophilic
addition
reaction
of
4-amino-4H-1,2,4-triazole
with
derivatives.
The
structure
compounds
verified
NMR,
IR
and
HRMS.
crystal
structures
TEMC-6
TEMC-12
determined
single-crystal
X-ray
diffraction
(XRD)
the
showed
presence
intermolecular
intramolecular
hydrogen
bonds
played
an
important
role
in
activity
effect.
vitro
antifungal
results
against
Wheat
gibberellic
that
methyl
alkoxy-substituted
had
good
biological
activity.
Among
them,
TEMC-7
best
effect
(EC50
=
6.74
μg/mL)
than
others
commercial
drug
fluconazole
(EC50=10.19
lasting
antibacterial
After
hyphae
growth
was
reached
to
a
certain
extent,
they
would
hardly
grow
again.
ranked
second,
their
bioactivity
significantly
better
triadimenol.
Molecular
docking
used
predict
binding
mode
ligands
CYP51
.
active
sites
included
coumarin
groups
residues
TRY
A:105,
triazole
ALA
A:291,
as
well
on
receptor
center
HEM
A:601,
achieving
at
least
three
different
ways
action.
substituent
TEMC-4
also
interacts
LEU
A:108
PHE
A:217,
nitrogen
atoms
interact
residue
SER
A:295,
ketone
lactone
ring
A:119,
increasing
interaction
protein.
Archiv der Pharmazie,
Год журнала:
2024,
Номер
357(4)
Опубликована: Янв. 21, 2024
Abstract
In
the
face
of
escalating
challenges
microbial
resistance
strains,
this
study
describes
design
and
synthesis
5‐({1‐[(1
H
‐1,2,3‐triazol‐4‐yl)methyl]‐1
‐indol‐3‐yl}methylene)thiazolidine‐2,4‐dione
derivatives,
which
have
demonstrated
significant
antimicrobial
properties.
Compared
with
minimum
inhibitory
concentrations
(MIC)
values
ciprofloxacin
on
respective
compounds
5a
,
5d
5g
5l
5m
exhibited
potent
antibacterial
activity
MIC
ranging
from
16
to
25
µM.
Almost
all
synthesized
showed
lower
compared
standards
against
vancomycin‐resistant
enterococcus
methicillin‐resistant
Staphylococcus
aureus
strains.
Additionally,
majority
remarkable
antifungal
activity,
Candida
albicans
Aspergillus
niger
as
nystatin,
griseofulvin,
fluconazole.
Furthermore,
notable
effects
Plasmodium
falciparum
strain,
having
IC
50
1.31
2.79
μM
standard
quinine
(2.71
μM).
Cytotoxicity
evaluation
5a–q
SHSY‐5Y
cells
at
up
100
μg/mL
no
adverse
effects.
Comparison
control
groups
highlights
their
noncytotoxic
characteristics.
Molecular
docking
confirmed
compound
binding
target
active
sites,
stable
protein–ligand
complexes
displaying
drug‐like
molecules.
dynamics
simulations
revealed
dynamic
stability
interactions.
Rigorous
tests
molecular
modeling
unveil
effectiveness
drug‐resistant
microbes,
providing
hope
for
new
potential
safety.
Pharmacological Research - Modern Chinese Medicine,
Год журнала:
2024,
Номер
10, С. 100405 - 100405
Опубликована: Фев. 25, 2024
Herbal
medicine,
including
Chinese
herbal
medicines
is
getting
attention
in
the
scientific
research
due
to
their
long
historical
applications
and
reliable
therapeutic
efficacy.
Coumarin
a
secondary
metabolites
found
be
present
different
species
of
plants.
Pteryxin
coumarin
Peucedanum
praeruptorum,
Pteryxia
terebinthina,
Radix
Peucedani,
Qian-Hu
Apiaceae
Present
paper
will
explore
highlights
key
information
pertaining
reported
activities
class
phytochemical
pteryxin.
In
work,
data
pteryxin
were
collected
from
Google,
Scopus,
PubMed,
Science
Direct
Google
Scholar
databases
using
keywords
coumarin,
The
various
sources
reveals
biological
potential
management
bone
loss,
seizures,
acute
lung
injury,
inflammatory
conditions,
Alzheimer's
disease,
hyperglycemia,
liver
uropathogenic
condition,
SARS-cov-2
infection.
Additionally,
also
possesses
vasorelaxant
antioxidant
activity.
this
analytical
aspects
like
separation,
isolation
identification
samples
has
been
discussed.
work
summarized
mechanistic
insights
into
medicinal
importance
translational
scope
for
treatment
human
disorders
associated
complications.
On
basis
existing
on
pteryxin,
it
may
concluded
that
there
need
rigorous
examine
through
preclinical
clinical
studies
its
as
lead
molecule.
explored
develop
functional
bioactive
molecules
structural
modification.
Critical Reviews in Analytical Chemistry,
Год журнала:
2025,
Номер
unknown, С. 1 - 21
Опубликована: Май 9, 2025
Indole
was
first
identified
around
1869,
this
being
an
indole
ring
system
which
is
a
fused
benzene
and
pyrrole
system.
Research
findings
illustrate
that
derivatives
have
gained
acceptance
as
therapeutic
agents
because
they
contain
structural
versatility
access
different
biological
targets.
Scientific
research
has
established
their
strong
pharmaceutical
properties,
especially
for
oncology
medicines
control
essential
cellular
processes
while
interrupting
defective
enzymatic
activities
of
topoisomerases,
kinases,
histone
deacetylases.
proves
indole-based
compounds
display
broad
antibacterial,
antifungal
antiparasitic
effects
in
addition
to
cancer-fighting
properties.
The
nucleus
creates
targeted
interactions
with
central
nervous
receptors
enzymes
visualization
neurological
delivery.
indicates
provide
benefits
managing
anti-inflammatory
responses
lowering
blood
pressure
diabetes
markers
although
benefiting
cardiovascular
health
through
ability
affect
specific
disease
pathways.
ongoing
development
optimization
methods
synthetic
improvements
leads
surpass
present
treatments
according
clinical
trials.
Structural
modifications
the
core
been
explored
recent
studies
improve
its
pharmacological
versatility.
from
2020
2024,
featuring
potency,
mechanism
action,
strategies
overcome
resistance,
highlighted,
focus
on
diseases.
Finds
databases
such
ScienceDirect,
Google
Scholar,
PubMed,
EMBASE
are
included
analysis.
Abstract
The
importance
of
indole‐based
heterocycle
scaffolds
in
medicinal
chemistry
has
increased
as
a
result
their
significant
pharmacological
and
biological
characteristics.
These
compounds′
the
discovery
creation
cutting‐edge
medications
to
treat
variety
diseases
is
an
instance
worth.
current
study
highlights
numerous
methods
available
create
different
favourable
medical
uses
with
literature
that
been
published
up
2023.
International Journal of Molecular Sciences,
Год журнала:
2023,
Номер
24(20), С. 15119 - 15119
Опубликована: Окт. 12, 2023
A
series
of
new
fluorinated
1-benzylisatins
was
synthesized
in
high
yields
via
a
simple
one-pot
procedure
order
to
explore
the
possible
effect
ortho-fluoro
(3a),
chloro
(3b),
or
bis-fluoro
(3d)
substitution
on
biological
activity
this
pharmacophore.
Furthermore,
isatins
could
be
converted
into
water-soluble
isatin-3-hydrazones
using
their
acid-catalyzed
reaction
with
Girard's
reagent
P
and
its
dimethyl
analog.
The
cytotoxic
action
these
substances
is
associated
induction
apoptosis
caused
by
mitochondrial
membrane
dissipation
stimulated
reactive
oxygen
species
production
tumor
cells.
In
addition,
compounds
3a
3b
exhibit
platelet
antiaggregation
at
level
acetylsalicylic
acid,
whole
fluorine-containing
does
not
adversely
affect
hemostasis
system
as
whole.
Among
pyridinium
isatin-3-acylhydrazones,
7c
5c,e
highest
antagonistic
against
phytopathogens
bacterial
fungal
origin
can
considered
useful
leads
for
combating
plant
diseases.
Journal of Saudi Chemical Society,
Год журнала:
2023,
Номер
27(6), С. 101761 - 101761
Опубликована: Окт. 27, 2023
The
skeleton
of
2-trifluoromethyl
quinoline
is
the
core
structure
many
natural
products
and
pharmaceutical
molecules.
synthesis
this
scaffold
limited
by
metal
catalysis,
harsh
conditions,
toxic
or
hazardous
reagents
solvents,
lower
atom-economy.
Herein,
a
novel
method
for
quinolines
via
[4+2]
cyclization
β-keto
esters
1,3-diketones
with
various
substituted
o-aminobenzaldehydes
using
free
catalyst
in
EOH
reported.
This
atom-
step-economical
protocol
features
simple
operation,
broad
substrate
scope,
good
functional-group
compatibility.
synthetic
utility
methodology
was
highlighted
easy
gram-scale
late-stage
functionalization,
which
would
promote
vigorous
development
chemistry.
Moreover,
vitro
antifungal
activities
against
F.
graminearum
(from
wheat),
corn),
moniliforme,
oxysporum,
R.
solani
were
investigated
to
further
potential
these
compounds.
PLoS ONE,
Год журнала:
2024,
Номер
19(7), С. e0305691 - e0305691
Опубликована: Июль 29, 2024
Trigonella
,
commonly
known
as
Fenugreek,
is
among
the
most
promising
medicinal
herbs
consumed
worldwide
due
its
protein
rich
dietary
contributions.
This
study
involved
induced
mutagenesis
on
two
species
(
foenum-graecum
var.
PEB
and
corniculata
Pusa
kasuri)
using
caffeine
sodium
azide
mutagens,
resulting
in
identification
of
nine
high-yielding
mutant
lines
M
3
generation.
Molecular
characterization
SCoT
markers
revealed
a
high
polymorphism
28.3%
46.7%
kasuri,
respectively,
facilitating
investigation
genetic
divergence
control
lines.
Similarity
correlation
analysis
indicated
similarity
between
A
C
(0.97)
J
O
(0.88),
while
lowest
was
observed
B
F
(0.74)
L
(0.58).
Mutant
displayed
highest
seed
yield
attributing
traits,
content
respectively.
Physiological
parameters,
including
chlorophyll
(Mutants
N)
carotenoids
(mutant
J),
exhibited
improvements.
Assessment
stomatal
characteristics
scanning
electron
microscopy
may
lead
to
improved
physiological
processes
distinction
at
interspecific
level,
Methanolic
extracts
both
were
subjected
GC-MS
analysis,
revealing
24
major
phytocompounds
for
their
pharmacological
activities
(antioxidant,
anti-inflammatory,
anticancer,
etc.).
Statistical
methods
such
Pearson
heatmap
pairwise
scatter
plot
matrix
provided
insights
into
correlations
linear
associations
parameters
kasuri.
The
strong
iron
seeds
per
pod
suggests
avenue
further
research.
Continued
research
breeding
efforts
these
mutants
can
significant
advancements
agriculture
medicine,
benefiting
farmers,
consumers,
industries
alike.
