Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 12, 2025
Rust
disease,
an
important
plant
pathogen,
can
lead
to
reduced
crop
or
fruit
production.
Trifluoromethyloxadiazole
(TFMO)
is
a
class
of
histone
deacetylase
inhibitors
(HDACs).
Herein,
series
5-(trifluoromethyl)-1,2,4-oxadiazole
(TFMO)-based
pyrimidin-4-ether
derivatives
were
designed
and
synthesized.
Antirust
bioassay
results
TFMOs
showed
that
some
them
possessed
excellent
activities
against
rust
pathogens,
such
as
Puccinia
sorghi,
Phakopsora
pachyrhizi,
rubigo.
The
most
active
compound,
3-(5-(((6-(difluoromethyl)pyrimidin-4-yl)oxy)methyl)thiophen-2-yl)-5-(trifluoromethyl)-1,2,4-oxadiazole
(XII6),
exhibited
50%
control
P.
pachyrhizi
at
0.780
mg/L,
which
was
significantly
better
than
the
commercial
fungicide
azoxystrobin
(0%)
same
concentration.
field
trial
indicated
compound
effect
rubigo
116
g
a.i./ha.
acute
toxic
XII6
has
low
toxicity.
Furthermore,
enzyme
activity
strong,
nonselective
HDAC
inhibitor.
Finally,
structure–activity
relationship
established,
XII6-HDAC
binding
mode
carried
out
based
on
crystal
structure
hHDAC1,
hHDAC4,
hHDAC6.
This
work
provided
for
further
optimization.
Journal of Agricultural and Food Chemistry,
Год журнала:
2024,
Номер
72(27), С. 15276 - 15283
Опубликована: Июнь 29, 2024
Using
nicofluprole
as
the
lead
compound,
we
designed
and
synthesized
a
series
of
new
phenylpyrazole
analogues
through
substituting
methyl
group
on
nitrogen
atom
amide
with
an
acyl
group.
Bioassay
results
showed
that
compounds
A12–A17
1-cyanocyclopropimide
exhibited
outstanding
insecticidal
activity.
The
LC50
values
for
against
Tetranychus
cinnabarinus
ranged
from
0.58
to
0.91
mg/L.
Compound
A15
value
0.29
3.10
mg/L
Plutella
xylostella
Myzus
persicae,
respectively.
Molecular
docking
indicated
potential
binding
interactions
compound
gamma-aminobutyric
acid
receptor.
Additionally,
density
functional
theory
calculations
implied
structure
might
be
essential
its
biological
Phenylpyrazole
derivatives,
containing
fragment,
have
further
development
insecticides.
Journal of Agricultural and Food Chemistry,
Год журнала:
2024,
Номер
72(32), С. 17802 - 17812
Опубликована: Авг. 2, 2024
Succinate
dehydrogenase
(SDH)
has
been
considered
an
ideal
target
for
discovering
fungicides.
To
develop
novel
SDH
inhibitors,
in
this
work,
31
benzothiazol-2-ylthiophenylpyrazole-4-carboxamides
were
designed
and
synthesized
using
active
fragment
exchange
a
link
approach
as
promising
inhibitors.
The
findings
from
the
tests
on
antifungal
activity
indicated
that
most
of
compounds
displayed
remarkable
inhibition
against
fungi
tested.
Compound
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.
Journal of Asian Natural Products Research,
Год журнала:
2025,
Номер
unknown, С. 1 - 14
Опубликована: Апрель 21, 2025
A
series
of
isoquinolone
compounds
Ia-Iq
containing
amide
moiety
were
rationally
designed
and
synthesized
based-on
alkaloids.
Their
structures
confirmed
by
1H
NMR,13C
NMR
HRMS.
Most
the
title
showed
medium
to
excellent
antifungal
activity
in
vitro
at
50
mg/L.
Especially,
EC50
Im
(13.155
mg/L)
against
P.
piricola
was
slightly
better
than
chlorothalonil
(14.323
mg/L).
The
vivo
on
apples
comparable
chlorothalonil.
Preliminary
mechanistic
exploration
illustrated
that
strongly
damage
mycelium
morphology.
Furthermore,
molecular
electrostatic
potential
docking
analysis
revealed
could
interact
with
residues
SDH
via
hydrogen
bond.
RSC Advances,
Год журнала:
2025,
Номер
15(20), С. 16088 - 16096
Опубликована: Янв. 1, 2025
Phenylpyrazole
derivatives
were
designed
and
synthesized
to
fabricate
novel
herbicides
containing
strobilurin
moieties.
Most
compounds
demonstrated
good
inhibition
on
A.
retroflexus
,
which
speculated
as
PPO
inhibitors.
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(11), С. 5345 - 5345
Опубликована: Июнь 2, 2025
In
response
to
the
urgent
need
for
innovative
fungicides
ensure
food
security
and
safety,
a
series
of
twenty-three
novel
trifluoromethylpyridine
compounds
were
designed
synthesized
using
scaffold
hopping
strategy
derived
from
dehydrozingerone.
This
approach
involved
converting
α,
β-unsaturated
ketone
moiety
into
pyridine
ring.
Bioassay
results
indicated
that
majority
these
exhibited
promising
in
vitro
antifungal
activity,
particularly
against
Rhizoctonia
solani
Colletotrichum
musae.
Notably,
compound
17
showed
highest
efficacy
broad-spectrum
with
median
effective
concentrations
(EC50)
ranging
2.88
9.09
μg/mL.
Phenoxytrifluoromethylpyridine
derivatives,
including
17,
superior
activity
compared
benzyloxytrifluoromethylpyridine
derivatives.
vivo
tests
revealed
both
23
moderate
control
effects
C.
The
degradation
half-lives
bananas
determined
be
176.9
h
94.8
h,
respectively,
indicating
stability
their
structures
environment.
Molecular
docking
studies
interacts
succinate
dehydrogenase,
offering
valuable
insights
structural
optimization
23.
