PLoS Pathogens,
Год журнала:
2024,
Номер
20(9), С. e1012544 - e1012544
Опубликована: Сен. 9, 2024
Anaplerosis
refers
to
enzymatic
reactions
or
pathways
replenishing
metabolic
intermediates
in
the
tricarboxylic
acid
(TCA)
cycle.
Pyruvate
carboxylase
(PYC)
plays
an
important
anaplerotic
role
by
catalyzing
pyruvate
carboxylation,
forming
oxaloacetate.
Although
PYC
orthologs
are
well
conserved
prokaryotes
and
eukaryotes,
their
pathobiological
functions
filamentous
pathogenic
fungi
have
yet
be
fully
understood.
Here,
we
delve
into
molecular
of
ortholog
gene
PYC1
Fusarium
graminearum
F.
oxysporum,
prominent
fungal
plant
pathogens
with
distinct
pathosystems,
demonstrating
variations
carbon
metabolism
for
pathogenesis.
Surprisingly,
deletion
mutant
oxysporum
exhibited
pleiotropic
defects
hyphal
growth,
conidiation,
virulence,
unlike
graminearum,
where
did
not
significantly
impact
virulence.
To
further
explore
species-specific
effects
on
pathogenicity,
conducted
comprehensive
profiling.
Despite
shared
changes,
reprogramming
central
nitrogen
was
identified.
Specifically,
alpha-ketoglutarate,
a
key
link
between
TCA
cycle
amino
metabolism,
showed
significant
down-regulation
exclusively
oxysporum.
The
response
associated
pathogenicity
notably
characterized
S-methyl-5-thioadenosine
S-adenosyl-L-methionine.
This
research
sheds
light
how
PYC1-mediated
anaplerosis
affects
reveals
variations,
exemplified
Journal of Agricultural and Food Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 18, 2024
Coumarin,
a
naturally
occurring
active
ingredient
with
various
biological
activities
in
pesticides,
is
commonly
found
plants
belonging
to
the
Rutaceae
and
Apiaceae
families.
Thanks
its
unique
structural
properties
natural
benefits,
coumarin
derivatives
exhibit
wide
range
of
physiological
activities,
including
insecticidal,
antifungal,
antibacterial,
herbicidal,
antiviral
properties.
These
compounds
have
attracted
considerable
interest
field
pesticide
development,
although
there
lack
comprehensive
reviews
on
their
use
pesticides.
This
Review
aims
provide
detailed
overview
applications
covering
structure–activity
relationship
analyses,
mechanisms
action.
It
hoped
that
this
will
offer
new
insights
into
discovery
these
development.
Organic Letters,
Год журнала:
2024,
Номер
26(33), С. 6993 - 6998
Опубликована: Авг. 8, 2024
Chiral
indoles
annulated
on
the
benzene
ring
are
unique
and
significant
in
natural
medicinal
compounds.
However,
accessing
these
enantioenriched
molecules
has
often
been
overlooked.
The
present
study
introduces
an
organocatalytic
protocol
to
access
compounds
efficiently,
demonstrated
by
substrate
scope,
functional
group
tolerance,
using
only
1
mol
%
of
a
chiral
conjugated
acid
catalyst.
Additionally,
explores
regioselectivity,
gram-scale
reactions,
follow-up
transformations,
underscoring
method's
potential.
Molecules,
Год журнала:
2025,
Номер
30(1), С. 172 - 172
Опубликована: Янв. 4, 2025
An
efficient
stereoselective
synthesis
of
10-hydroxy-10-(1H-indol-3-yl)-9-(10H)-phenanthrene
derivatives
was
realized
through
an
organocatalyzed
Friedel–Crafts
reaction
phenanthrenequinones
and
indoles
using
a
(S,S)-dimethylaminocyclohexyl-squaramide
as
the
catalyst.
Under
optimized
conditions,
desired
chiral
products
were
obtained
in
good
yields
(73–90%)
with
moderate
to
high
ee
values
(up
97%
ee).
Two
pairs
synthesized
enantiomers
subjected
evaluation
their
antiproliferative
activities
on
four
types
human
cancer
cell
lines
one
umbilical
vein
endothelial
line
CCK-8
assay.
The
results
indicated
that
stereoselectivity
had
obvious
impacts
biological
activity.
(S)-4g
found
have
optimal
cytotoxicity
against
A549
safety
profile
for
normal
cells,
which
better
than
inhibitory
activity
positive
control
drug
(doxorubicin).
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 27, 2025
The
discovery
of
novel
leads
and
new
targets
is
an
important
approach
to
address
the
issue
fungicide
resistance
by
development.
indole
skeleton
has
been
widely
utilized
in
agrochemicals
due
its
unique
biological
activity.
YZK-C22
a
potent
pyruvate
kinase
inhibitor
with
high
antifungal
Several
were
developed
based
on
YZK-C22.
Inspired
these,
[1,2,4]triazino[4,5-a]indol-1(2H)-one
derivatives
designed
using
hopping
strategy;
however,
these
compounds
exhibited
moderate
fungicidal
Unexpectedly,
2-(1H-indol-2-yl)-1,3,4-oxadiazole
formed
under
controlled
reaction
conditions
showed
significantly
higher
Compounds
6c,
6d,
6f,
6j
excellent
activity
vitro,
EC50
values
ranging
from
0.120
0.310
μg/mL
against
Botrytis
cinerea,
more
than
commercial
pyrimethanil
(EC50
=
0.990
μg/mL).
In
field
trials
at
540
720
g
active
ingredient
(ai)/hm2,
compound
6c
81.46
86.58%
efficacy
B.
that
rate
ai/hm2
(70.46%).
affinity
constants
6d
cinerea
lower
Higher
but
implies
may
work
as
prodrugs
or
have
different
mode
action.
Thus,
are
worth
being
further
investigated.
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 Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 13, 2025
The
isoxazoline
insecticide,
such
as
fluralaner,
exhibits
strong
insecticidal
activity
against
pests
while
showing
no
cross-resistance.
However,
due
to
its
toxicity
bees,
the
use
of
Fluralaner
is
restricted
in
veterinary
antiparasitic
applications.
Hence,
how
modify
structure
fluralaner
maintain
and
reduce
bees
vital
meaningful.
In
this
study,
a
virtual
screening
11
diamide
substructures
was
conducted
based
on
GABA
receptor
(Apis
mellifera),
four
compounds
with
lower
docking
scores
were
regarded
potential
low
bee
compounds.
Among
them,
compound
Y11
containing
thiophene
diamine
motif
used
lead
compound.
Subsequently,
A1-A16
B1-B11
synthesized
Y11.
Interestingly,
A13
exhibited
LC50
values
1.4
μg/mL
diamondback
moth
(Plutella
xylostella),
outperforming
commercial
insecticide
ethiprole
(LC50
=
2.9
μg/mL).
Furthermore,
9.9
fall
armyworm
(Spodoptera
frugiperda),
also
Fipronil
78.8
Compound
B1
12.4
corn
borer
(Pyrausta
nubilalis),
which
surpassed
that
(30.8
Although
P.
xylostella
S.
frugiperda
not
potent
Fluralaner,
only
1/200
Fluralaner.
Molecular
dynamics
studies
elucidated
interaction
mode
bee.
has
serve
candidate
low-toxicity
alternative
offering
valuable
insights
for
future
design
insecticide.
