Unveiling the Cyclopropyl Appended Acyl Thiourea Derivatives as Antimicrobial, α-Amylase and Proteinase K Inhibitors: Design, Synthesis, Biological Evaluation, Molecular Docking, DFT and ADMET Studies
Archives of Biochemistry and Biophysics,
Год журнала:
2025,
Номер
unknown, С. 110304 - 110304
Опубликована: Янв. 1, 2025
Язык: Английский
Design, synthesis, and antibacterial activity of novel amide derivatives containing a sulfone moiety
Molecular Diversity,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 11, 2025
Язык: Английский
Discovery of Novel Amide Derivatives Containing an Oxazole/Isoxazole Moiety as Potential SDH Inhibitors: Design, Synthesis, and Nematicidal Activity
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 25, 2025
To
develop
new
nematicides,
amide
derivatives
with
oxazole/isoxazole
were
synthesized
via
scaffold-hopping
as
succinate
dehydrogenase
(SDH)
inhibitors.
The
nematicidal
activities
of
these
target
compounds
tested
against
Bursaphelenchus
xylophilus,
Aphelenchoides
besseyi,
and
Ditylenchus
destructor.
Some
the
showed
excellent
activities.
Compound
B21
had
LC50
values
3.2
mg/L
for
B.
11.5
A.
10.5
D.
exerted
a
pronounced
inhibitory
effect
on
feeding,
reproduction,
embryonic
development
capabilities
while
concurrently
triggering
deleterious
oxidative
stress
responses
within
nematodes.
These
reactions
led
to
intestinal
damage
eventually
death
exhibited
strong
hydrophobic
interactions
residues
Arg-76,
Val-103,
Pro-193,
Ile-242
SDH.
Additionally,
significantly
inhibited
SDH
an
IC50
value
6.5
μmol/L.
Язык: Английский
Design, Synthesis, and Nematicidal Activity of Novel Amide Derivatives Containing an 1,2,4/1,3,4-Oxadiazole Moiety against Bursaphelenchus xylophilus
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 12, 2025
To
discover
novel
structural
nematicides,
79
amide
compounds
containing
1,2,4/1,3,4-oxadiazole
moiety
were
designed,
synthesized,
and
evaluated
for
nematicidal
efficacy
against
second-stage
juveniles
of
Bursaphelenchus
xylophilus
(B.
xylophilus).
Notably,
some
exhibited
superior
efficacy,
example,
the
LC50
values
11,
39,
40,
48,
49,
51,
52,
54
7.4,
31.0,
35.3,
10.3,
12.7,
6.9,
21.5,
52.2
mg/L,
respectively,
with
activities
significantly
surpassing
that
tioxazafen
(79.3
mg/L).
Compound
51
multifaceted
activity
through
suppression
motility,
feeding,
reproduction,
combined
induction
oxidative
stress.
reduced
nematode
protein
content
impaired
antioxidant
capacity.
Meanwhile,
compound
demonstrates
binding
energy
interaction
mode
succinate
dehydrogenase
(SDH),
showing
potent
SDH
inhibition
(IC50
=
15.0
μmol/L).
Therefore,
which
may
become
a
potential
inhibitor,
interferes
metabolism
by
inhibiting
activity,
resulting
in
death.
Язык: Английский
Eco-Innovative Pesticide Discovery via Conformation Restriction Strategy: Balancing Efficacy and Environmental Safety
Journal of Molecular Structure,
Год журнала:
2025,
Номер
unknown, С. 142304 - 142304
Опубликована: Апрель 1, 2025
Язык: Английский
Novel amide derivatives containing an 1,2,4‐oxadiazole moiety as potential SDH inhibitors: design, synthesis, and nematicidal activity
Pest Management Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 5, 2025
Abstract
BACKGROUND
The
pine
wilt
disease
(PWD)
caused
by
Bursaphelenchus
xylophilus
is
considered
the
‘cancer’
of
trees,
and
protecting
forests
from
destructive
impact
nematode
remains
a
significant
challenge.
Chemical
control
one
most
effective
methods
for
managing
plant
nematodes.
Developing
new
nematicides
an
strategy
urgent
need
management.
RESULTS
Amide
derivatives
containing
1,2,4‐oxadiazole
were
designed
synthesized
through
scaffold‐hopping
strategy.
Some
target
compounds
exhibited
nematicidal
activities.
For
example,
compound
F3
showed
half‐maximal
lethal
concentration
(LC
50
)
value
3.63
mg/L
against
.
Compound
not
only
significantly
inhibited
hatching
eggs,
but
also
reduced
feeding,
reproduction,
motility
Additionally,
induced
accumulation
lipofuscin,
lipids,
reactive
oxygen
species
(ROS)
in
,
leading
to
harmful
oxidative
stress
responses.
severe
damage
intestinal
barrier,
led
shrinkage
surface.
Interestingly,
favorable
interaction
pattern
with
succinate
dehydrogenase
(SDH)
was
similar
fluopyram
SDH.
may
inhibit
activity
SDH,
blockage
electron
transfer
respiratory
chain,
thereby
resulting
death.
CONCLUSION
can
serve
as
potential
lead
SDH
inhibitor,
further
molecular
structure
optimization
discover
future.
©
2025
Society
Industry.
Язык: Английский
Discovery of novel nematicidal active ingredient 2,4,7-trichloroquinazoline as a potential SDH inhibitor
Physiological and Molecular Plant Pathology,
Год журнала:
2024,
Номер
unknown, С. 102433 - 102433
Опубликована: Окт. 1, 2024
Discovery and Mechanism of 1,4-Dichloropyrido[3,4-D]Pyridazine as a Potential Nematicidal Candidate
Опубликована: Янв. 1, 2024
Язык: Английский
Tetramycin B3: An Effective and Biological Nematicide for Bursaphelenchus xylophilus
Forests,
Год журнала:
2024,
Номер
15(10), С. 1699 - 1699
Опубликована: Сен. 26, 2024
Pine
wilt
disease,
caused
by
Bursaphelenchus
xylophilus
(Steiner
&
Buhrer,
1934)
Nickle
1981,
poses
a
significant
threat
to
the
safety
of
pine
forests
in
world.
Currently,
available
nematicides
for
controlling
this
disease
are
limited.
Finding
new
is
crucial
effective
prevention
and
control
disease.
In
study,
we
discovered
that
tetramycin
B3,
derived
from
Streptomyces
ahygroscopicus,
demonstrated
promising
effect
on
The
LC50
values
B3
at
24,
48,
72
h
were
26.49,
23.37,
12.79
μg/mL,
respectively.
Tetramycin
significantly
inhibited
feeding
growth
rate
B.
low
concentrations
while
also
increasing
ROS
(reactive
oxygen
species)
production
lipid
accumulation.
Furthermore,
markedly
activity
detoxifying
protective
enzymes.
Transcriptome
metabolome
analyses
indicated
affected
expression
genes
related
lysosomes,
autophagy,
metabolism
xylophilus.
Additionally,
delayed
onset
results
showed
influenced
defense
responses
trees
induced
produce
disease-resistant
mechanisms.
Future
research
will
focus
further
elucidating
mechanism
action
against
verifying
gene
functions
identified
through
transcriptome
screening.
Язык: Английский
Discovery and Mechanism of 1,4-Dichloropyrido[3,4-d]pyridazine as a Potential Nematicidal Candidate
ACS Agricultural Science & Technology,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 25, 2024
Plant
nematode
disease
management
is
still
a
difficult
problem
in
agricultural
production.
To
develop
novel
green
nematicides,
pyridazine
compounds
with
nematicidal
activities
against
Ditylenchus
destructor
(D.
destructor),
Bursaphelenchus
xylophilus
(B.
xylophilus),
Aphelenchoides
besseyi
(A.
besseyi),
and
Meloidogyne
incognita
(M.
incognita)
were
discovered.
The
LC50
values
of
compound
C2
7.1
3.4
mg/L
D.
A.
besseyi,
respectively.
Compound
not
only
caused
an
adverse
oxidative
stress
response
nematodes,
resulting
intestinal
damage,
but
also
significantly
inhibited
egg
hatching
destructor.
may
lead
to
decreased
cellular
tolerance
antioxidant
function
by
downregulating
the
differential
gene
heat
shock
70
kDa
protein,
thereby
accelerating
cell
litter
process
ultimately
leading
death
nematode.
can
serve
as
potential
nematicide
worthy
further
study
future.
Язык: Английский