Thin layer chromatography assay to detect laccase inhibitors
Food Chemistry,
Год журнала:
2024,
Номер
460, С. 140583 - 140583
Опубликована: Июль 24, 2024
Язык: Английский
Discovery of novel flavonoid derivatives containing benzothiazole as potential antifungal agents
Pest Management Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 8, 2025
Abstract
BACKGROUND
Fungal
diseases
of
plants
have
a
serious
impact
on
the
quality
and
yield
crops,
some
traditional
pesticides
can
no
longer
cope
with
this
problem.
Therefore,
it
is
great
significance
to
develop
new
high
efficiency
low
toxicity.
RESULTS
A
series
flavonoid
derivatives
containing
benzothiazole
were
designed
synthesized.
Among
them,
compounds
V17
,
V12
V13
had
excellent
inhibitory
effect
against
Fusarium
oxysporum
f.
sp.
cucumerinu
half‐maximal
concentration
(EC
50
)
values
1.2,
2.3,
3.2
μg/mL,
which
better
than
control
drug
Kresoxim‐methyl
(
Km
37.8
μg/mL).
The
in
vivo
protective
activity
curative
activities
cucumber
fusarium
wilt
caused
by
F.
cucumerinum
82.4
60.5%
at
200
(60.2
48.6%).
In
addition,
could
damage
cell
membrane
mycelia,
be
confirmed
determination
cytoplasmic
leakage,
detection
permeability,
measurement
malondialdehyde
(MDA).
Similarly,
scanning
electron
microscopy
(SEM)
experiment
optical
microscope
characterization
provide
direct
evidence
for
destruction
mycelium
treated
.
CONCLUSION
significantly
reduced
pathogenicity
provided
idea
direction
development
green
pesticides.
©
2025
Society
Chemical
Industry.
Язык: Английский
Thiourea Derivatives in Agrochemical Discovery and Development
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 7, 2025
Thiourea,
represented
by
the
chemical
formula
(R1R2N)(R3R4N)C═S,
is
a
significant
organic
sulfur
compound
characterized
presence
of
atom
and
two
amino
groups.
Meanwhile,
thiourea
isothiourea
are
reciprocal
isomers.
This
structure
facilitates
formation
biologically
active
moiety,
which
interconnected
through
double
bonds
between
nitrogen
atoms.
As
potent
component
in
pesticide
formulations,
demonstrates
efficacy
safeguarding
crops
against
variety
diseases
inhibiting
growth
reproduction
pathogens.
review
aims
to
provide
comprehensive
summary
derivatives
exhibiting
fungicidal,
insecticidal,
antiviral,
herbicidal,
plant
regulatory
properties,
with
objective
offering
new
perspectives
for
identifying
innovative
thiourea-based
pesticides
elucidating
their
mechanisms
action.
Язык: Английский
Design, Synthesis, Antifungal Evaluation, and Action Mechanism of Novel l-Carvone-Based Derivatives as Potential Succinate Dehydrogenase Inhibitors
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 16, 2025
Natural
products
serve
as
a
crucial
source
of
compounds
for
developing
novel
agricultural
antifungals.
In
this
work,
we
utilized
the
natural
product
l-carvone
molecular
scaffold
to
design
and
synthesize
three
series
l-carvone-based
derivatives.
The
in
vitro
bioassay
results
indicated
that
most
target
exhibited
remarkable
antifungal
activity.
Notably,
compound
C3
demonstrated
broad-spectrum
activity
against
Rhizoctonia
solani,
Botrytis
cinerea,
Sclerotinia
sclerotiorum,
Gibberella
zeae,
Valsa
mali,
with
EC50
values
0.274,
0.985,
4.17,
5.71,
2.29
μg/mL,
respectively.
vivo
preventative
efficacies
C11
R.
solani
C13
B.
cinerea
revealed
they
had
potential
mechanism
study,
cell
membrane
permeability
experiment
showed
significantly
increased
membrane,
microscopic
observations
could
destroy
structural
integrity
cells
reduce
number
mitochondria,
thus
affecting
normal
growth
mycelia.
Furthermore,
mitochondrial
detection,
succinate
dehydrogenase
(SDH)
enzyme
assay,
dynamics
(MD)
simulations,
docking
experiments
further
action
binding
mode
SDH
may
be
similar
those
thifluzamide.
abovementioned
provided
valuable
reference
discovery
inhibitor
fungicides.
Язык: Английский
Design, synthesis, antifungal evaluation and mechanism study of myrtenal derivatives as potential laccase inhibitors
Pest Management Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 15, 2025
Abstract
BACKGROUND
To
develop
novel
natural
product‐derived
fungicides,
four
series
of
myrtenal
oxadiazole/thiadiazole‐hydrazide/amide
derivatives
were
designed,
synthesized
and
evaluated
for
their
inhibitions
toward
several
crop
pathogenic
fungi/oomycetes.
RESULTS
In
the
in
vitro
antifungal
experiments,
some
showed
good
activity
against
Botryosphaeria
dothidea,
Sclerotinia
sclerotiorum
Fusarium
graminearum
.
Among
them,
compound
6d
exhibited
best
B.
dothidea
,
with
EC
50
value
0.052
mg/L,
which
was
significantly
stronger
than
carbendazim
(EC
=
0.40
mg/L).
vivo
assay
on
apple
fruits
branches
that
displayed
significant
protective
curative
effects,
both
superior
to
carbendazim.
preliminary
mechanism
study,
can
damage
surface
morphology
mycelia,
destroy
integrity
permeability
cell
membrane,
increase
intracellular
ROS
content,
thereby
inhibiting
growth
Compound
also
inhibited
laccase
IC
8.45
μM,
much
cysteine
PMDD‐5Y.
Molecular
docking
confirmed
binding
affinity
interaction
mode
laccase.
CONCLUSION
This
study
presented
a
promising
lead
inhibitors
as
fungicidal
agrochemicals,
demonstrated
anti‐
inhibitory
activity.
©
2025
Society
Chemical
Industry.
Язык: Английский
Discovery of novel 4‐sulfur‐substituted pyrazol‐5‐yl‐benzamide derivatives containing amide/hydrazide/ester moieties as potential succinate dehydrogenase inhibitors
Pest Management Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Июнь 2, 2025
Abstract
BACKGROUND
Succinate
dehydrogenase
inhibitor
(SDHI)
fungicides
have
been
widely
utilized
in
the
combat
of
plant
pathogenic
fungi
due
to
their
potent,
broad‐spectrum
antifungal
activity
and
unique
mode
action.
In
this
study,
a
series
novel
4‐sulfur‐substituted
pyrazol‐5‐yl‐benzamide
derivatives
containing
amide,
hydrazide,
or
ester
moieties
were
synthesized
develop
innovative
SDH
inhibitors.
RESULTS
The
bioassay
studies
indicated
that
several
compounds
exhibited
potent
vitro
fungicidal
against
various
fungi.
Particularly,
compound
4d
demonstrated
efficacy,
with
EC
50
values
0.21,
0.95,
0.64,
1.33,
0.66
mg
L
−1
Valsa
mali
,
Botrytis
cinerea
Rhizoctonia
solani
Fusarium
graminearum
Gaeumannomyces
graminis
respectively.
vivo
effectively
prevented
V.
infection
apples
at
showing
superior
protective
curative
effects
(93.4%
85.5%)
compared
lead
A27
(68.7%
57.0%)
commercial
fungicide
fluxapyroxad
(55.4%
43.6%).
Enzymatic
inhibition
assays
molecular
docking
analysis
suggested
could
serve
as
potential
inhibitor.
CONCLUSION
This
study
offers
valuable
insights
for
expanding
spectrum
further
developing
them
©
2025
Society
Chemical
Industry.
Язык: Английский
Evaluation of the antifungal activity of novel bis-pyrazole carboxamide derivatives and preliminary investigation of the mechanism
Bioorganic Chemistry,
Год журнала:
2024,
Номер
153, С. 107779 - 107779
Опубликована: Сен. 1, 2024
Язык: Английский
l-Isoleucine-Derived Amide-hydrazide Compounds Evaluated as a Novel Potential Agricultural Fungicide
Journal of Agricultural and Food Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 18, 2024
Building
upon
previous
structure–activity
relationships
about
the
fungicidal
amide
and
hydrazide
lead
structures,
24
novel
amide-hydrazide
compounds
were
designed
synthesized
with
L-isoleucine
as
initial
skeleton
to
explore
impact
of
substituents
in
bridge
on
activity.
Among
these
compounds,
A5
exhibited
excellent
broad
spectrum
inhibitory
activity,
along
satisfactory
vivo
protective
efficiency
against
R.
solani
at
concentrations
200
50
μg·mL–1.
Scanning
electron
microscopy
(SEM)
transmission
(TEM)
observations
revealed
that
compound
induced
significant
morphological
changes
mycelium
coupled
vacuole
rupture
cytoplasmic
inhomogeneity
cellular
structures.
Transcriptomic
metabolomic
analyses
indicated
that,
following
treatment,
differentially
expressed
genes
metabolites
significantly
enriched
carbohydrate
metabolism-related
pathways
well
lipid
metabolism-associated
pathways,
including
glycerophospholipid
metabolism,
steroid
biosynthesis,
arachidonic
acid
sphingolipid
metabolism.
Additionally,
demonstrated
low
toxicity
zebrafish,
survival
rates
100%
60%
1
10
μg·mL–1,
respectively,
over
a
period
7
days.
The
above
results
provide
theoretical
guidance
for
development
green
candidates.
Язык: Английский