Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 26, 2024
The
γ-butyrolactone
scaffold,
commonly
present
in
natural
products
and
bioactive
compounds,
has
played
a
crucial
role
the
development
of
novel
pesticides.
In
this
study,
series
α-methylene-γ-butyrolactone
derivatives
containing
diphenyl
ether
moiety
were
designed
synthesized
using
scaffold
splicing
strategy.
Bioassays
revealed
that
several
target
compounds
demonstrated
potent
fungicidal
activities,
particularly
against
Phytophthora
capsici
Valsa
mali.
Notably,
compound
B7
(EC50
=
0.809
mg/L)
exhibited
highest
antioomycete
activity
P.
capsici,
outperforming
famoxadone
41.0
but
being
less
effective
than
dimethomorph
0.180
mg/L).
Meanwhile,
C22
1.47
showed
strongest
antifungal
V.
mali,
which
was
higher
those
1.80
13.6
vivo
experiments
confirmed
satisfactory
protective
curative
effects
better
famoxadone.
Additionally,
found
to
inhibit
sporangia
formation,
zoospore
release,
cystospore
germination
at
10
mg/L.
Physiological
biochemical
studies
indicated
can
induce
changes
mycelial
morphology
increase
cell
membrane
permeability,
modulate
respiratory
metabolism.
Furthermore,
both
vitro
enzymatic
inhibition
assays
molecular
docking
analysis
suggested
primary
mechanism
action
may
involve
binding
complex
III
on
chain.
This
work
provides
valuable
insights
for
incorporating
as
agricultural
agents.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(20), P. 11331 - 11340
Published: May 9, 2024
Research
on
mesoionic
structures
in
pesticide
design
has
gained
significant
attention
recent
years.
However,
the
1-position
of
pyridino[1,2-a]pyrimidine
is
usually
designed
with
2-chlorothiazole,
2-chloropyridine,
or
cyano
moieties
commonly
found
neonicotinoid
insecticides.
In
order
to
enrich
available
pharmacophore
library,
here,
we
disclose
a
series
new
mesoionics
bearing
indole-containing
substituents
at
1-position.
Most
these
target
compounds
are
confirmed
have
good
insecticidal
activity
against
aphids
through
bioevaluation.
addition,
three-dimensional
structure–activity
relationship
model
established
allow
access
optimal
compound
F45
an
LC50
value
2.97
mg/L.
This
comparable
property
achieved
by
positive
control
triflumezopyrim
(LC50
=
2.94
mg/L).
Proteomics
and
molecular
docking
analysis
suggest
that
potential
modulate
functioning
aphid
nervous
system
its
interaction
neuronal
nicotinic
acetylcholine
receptors.
study
expands
existing
library
for
future
development
insecticides
based
modifications
scaffold.
Journal of Agricultural and Food Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 7, 2025
Lepidopteran
species
cause
significant
harm
to
agricultural
yields
and
food
quality.
In
this
study,
a
series
of
innovative
isoxazoline
derivatives
incorporating
pyrazolamide
moieties
were
carefully
designed
synthesized
as
potential
insecticidal
agents.
Among
these,
compound
F16
demonstrated
an
LC50
value
0.01
mg/L
against
Plutella
xylostella,
surpassing
that
the
lead
fluxametamide
(LC50
=
0.15
mg/L).
Furthermore,
exhibited
broad-spectrum
activity
Pyrausta
nubilalis,
Spodoptera
frugiperda,
Chilo
suppressalis,
Aphis
craccivora,
Sogatella
furcifera.
Notably,
possessed
low
toxicity
Danio
rerio,
whereas
displayed
moderate
toxicity.
molecular
docking
analysis
potent
is
likely
mediated
by
its
specific
interactions
with
γ-GABA
receptors
primarily
through
formation
hydrogen
bonds
key
residues.
Density
functional
theory
calculations
electrostatic
potentials
also
performed
gain
insights
into
behavior
F16.
These
findings
suggest
promising
candidate
for
further
investigation
novel
pesticide.
Journal of Agricultural and Food Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: April 3, 2025
Isoxazolines
are
five-membered
heterocycle
compounds
with
a
wide
range
of
pharmacological
and
pesticidal
activities.
Numerous
marketed
pesticides
contain
an
isoxazoline
motif
as
key
skeleton.
Isoxazoline
have
relatively
simple
syntheses
biological
activities
against
various
weeds,
bacteria,
other
pests.
In
recent
years,
they
received
increasing
attention
widely
used
in
organic
chemistry
research,
such
intermediate
catalyst
ligands
synthesis.
They
also
excellent
optoelectronic
properties
the
field
materials.
Hence,
exploration
derivatives
remains
important
research
area
pesticide
discovery.
This
review
provides
up-to-date
overview
utilized
discovery,
highlighting
their
structure
properties.
It
summarizes
relevant
publications
from
last
10
offering
insights
into
advancements
this
research.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(27), P. 15077 - 15091
Published: June 26, 2024
In
recent
decades,
the
unique
structural
attributes
and
purported
insecticidal
properties
of
oximes
have
garnered
increasing
attention.
A
variety
insecticides,
encompassing
fluxametamide,
fluhexafon,
lepimectin,
been
synthesized,
all
which
incorporate
oximes.
This
review
endeavors
to
encapsulate
efficacy,
structure-activity
correlations,
operative
mechanisms
oxime-containing
compounds.
Furthermore,
it
delves
into
conceptual
frameworks
underpinning
design
innovative
oxime-based
thereby
shedding
light
on
prospective
advancements
in
this
field.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(44), P. 24847 - 24856
Published: Oct. 23, 2024
In
recent
years,
isoxazole
insecticides
or
parasiticides
targeting
the
γ-aminobutyric
acid
receptor,
such
as
fluralaner
fluxametamide,
featured
a
novel
chemical
structure
and
exhibited
potent
insecticidal
activity
with
no-cross
resistance.
Thus,
many
research
institutes
have
tried
to
modify
structures
of
these
agents
find
new
insecticide.
Previously,
majority
researchers
stuck
"phenyl-isoxazole-phenyl"
structure,
making
modifications
only
other
components.
this
study,
ternary
motif
was
modified
for
first
time
based
on
bioisosterism
theory.
A
series
derivatives
carrying
pyrazoline
1,3,4-oxadiazole
moieties
were
designed
synthesized
investigate
their
activities
against
diamondback
moth
(
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(38), P. 20974 - 20980
Published: Sept. 16, 2024
The
long-term
use
of
agricultural
insecticides
has
led
to
the
development
resistant
strains.
In
this
context,
isoxazoline
structure
become
an
active
area
pesticide
research
owing
its
wide
insecticidal
spectrum,
nontoxicity
mammals,
and
lack
cross-resistance
with
known
insecticides.
present
study,
based
on
discovery
compound
Chemistry & Biodiversity,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Oct. 27, 2024
Abstract
A
series
of
innovative
benzo[4,5]imidazo[1,2‐
b
]pyrazole
scaffold
containing
compounds
were
rationally
designed
through
a
ring‐closure
hopping
strategy
and
synthetized
with
an
intermediate
derivatization
approach.
Physicochemical
properties
analysis
indicated
the
potential
pesticide‐likeness
target
compounds.
The
optimal
compound
A14
showed
relatively
good
insecticidal
activity
against
P.
xylostella
,
LC
50
value
37.58
mg/L,
demonstrated
lower
acute
fish
toxicity
compared
to
fipronil.
Docking
binding
mode
that
bound
GABAR
H‐bond
between
amide
group
residue
6’Thr.
differences
in
modes
fipronil
may
be
key
factor
for
reduced
activities.
elucidated
SAR
profile
lay
foundation
further
structural
optimization
derivatives.
