ACS Synthetic Biology,
Journal Year:
2024,
Volume and Issue:
13(9), P. 2982 - 2991
Published: Sept. 9, 2024
Phenazine-based
small
molecules
are
nitrogen-containing
heterocyclic
compounds
with
diverse
bioactivities
and
electron
transfer
properties
that
exhibit
promising
applications
in
pharmaceutical
electrochemical
industries.
However,
the
biosynthetic
mechanism
of
highly
substituted
natural
phenazines
remains
poorly
understood.
In
this
study,
we
report
direct
cloning
heterologous
expression
lomofungin
gene
cluster
(BGC)
from
Chemical Biology & Drug Design,
Journal Year:
2025,
Volume and Issue:
105(1)
Published: Jan. 1, 2025
ABSTRACT
Invasive
fungal
infections
(IFIs)
pose
significant
challenges
in
clinical
settings,
particularly
due
to
their
high
morbidity
and
mortality
rates.
The
rising
incidence
of
these
infections,
coupled
with
increasing
antifungal
resistance,
underscores
the
urgent
need
for
novel
therapeutic
strategies.
Current
drugs
target
cell
membrane,
wall,
or
intracellular
components,
but
resistance
mechanisms
such
as
altered
drug‐target
interactions,
enhanced
efflux,
adaptive
cellular
responses
have
diminished
efficacy.
Recent
research
has
highlighted
potential
dual
inhibitors
that
simultaneously
multiple
pathways
enzymes
involved
growth
survival.
Combining
pharmacophores,
lanosterol
14α‐demethylase
(CYP51),
heat
shock
protein
90
(HSP90),
histone
deacetylase
(HDAC),
squalene
epoxidase
(SE)
inhibitors,
led
development
compounds
activity
reduced
resistance.
This
dual‐target
approach,
along
chemical
scaffolds,
not
only
represents
a
promising
strategy
combating
is
also
being
utilized
anticancer
agents.
review
explores
new
agents
employ
mono‐,
dual‐,
multi‐target
strategies
combat
IFIs.
We
discuss
emerging
targets,
mechanisms,
innovative
approaches
offer
hope
managing
challenging
infections.
Journal of Saudi Chemical Society,
Journal Year:
2023,
Volume and Issue:
28(2), P. 101797 - 101797
Published: Dec. 23, 2023
A
series
of
flavonoid
derivatives
containing
1,2,4-triazolo[4,3-a]pyridine
were
designed,
synthesized
and
evaluated
for
their
antifungal
activity.
Bioactivity
tests
showed
that
some
target
compounds
exhibited
the
strong
activity
against
Botrytis
cinerea
(B.
cinerea),
Sclerotinia
sclerotiorum
(S.
sclerotiorum),
Phomopsis
sp.
Among
them,
half
maximal
effective
concentration
(EC50)
value
S2
B.
was
3.3
μg/mL,
which
less
than
control
drug
azoxystrobin
(21.0
μg/mL).
The
EC50
S.
12.7
better
(28.1
In
addition,
in
vivo
protective
curative
activities
blueberry
92.0
79.8
%
at
200
respectively,
higher
those
(89.4
71.7%).
Scanning
electron
microscopy
(SEM)
spore
germination
experiments
could
not
only
cause
mycelium
damage
but
also
inhibited
germination.
Fluorescence
(FM)
observation,
relative
electrical
conductivity
measurement
cytoplasmic
leakage
assays
indicated
affect
cell
membrane
integrity
by
inducing
lipid
peroxidation
increasing
permeability
as
well
causing
contents.
These
results
show
had
excellent
inhibitory
effects
on
cinerea,
providing
another
supplement
development
new
pesticides.
Journal of Fungi,
Journal Year:
2024,
Volume and Issue:
10(5), P. 334 - 334
Published: May 5, 2024
Fungi
are
eukaryotic
organisms
with
relatively
few
pathogenic
members
dangerous
for
humans,
usually
acting
as
opportunistic
infections.
In
the
last
decades,
several
life-threatening
fungal
infections
have
risen
mostly
associated
worldwide
extension
of
chronic
diseases
and
immunosuppression.
The
available
antifungal
therapies
cannot
combat
this
challenge
because
arsenal
compounds
is
scarce
displays
low
selective
action,
significant
adverse
effects,
increasing
resistance.
A
growing
isolation
outbreaks
triggered
by
species
formerly
considered
innocuous
being
recorded.
From
ancient
times,
natural
substances
harvested
from
plants
been
applied
to
folk
medicine
some
them
recently
emerged
promising
antifungals.
most
used
briefly
revised
herein.
Combinations
chemotherapeutic
drugs
products
obtain
more
efficient
gentle
treatments
also
revised.
Nevertheless,
considerable
research
work
still
necessary
before
their
clinical
use
can
be
generally
accepted.
Many
a
highly
complex
chemical
composition,
active
principles
partially
unknown.
Here,
we
survey
field
underlying
lights
shadows
both
groups.
More
studies
involving
strains
necessary,
but
illustrate
matter
discussing
potential
applications
combined
carnosic
acid
plus
propolis
formulations.
Journal of Pineal Research,
Journal Year:
2024,
Volume and Issue:
76(4)
Published: May 1, 2024
Abstract
Natural
products,
known
for
their
environmental
safety,
are
regarded
as
a
significant
basis
the
modification
and
advancement
of
fungicides.
Melatonin,
low‐cost
natural
indole,
exhibits
diverse
biological
functions,
including
antifungal
activity.
However,
its
potential
an
agent
has
not
been
fully
explored.
In
this
study,
series
melatonin
derivatives
targeting
mitogen‐activated
protein
kinase
(Mps1)
fungal
pathogens
were
synthesized
based
on
properties
melatonin,
among
which
trifluoromethyl‐substituted
derivative
Mt‐23
exhibited
activity
against
seven
plant
pathogenic
fungi,
effectively
reduced
severity
crop
diseases,
rice
blast,
Fusarium
head
blight
wheat
gray
mold
tomato.
particular,
EC
50
(5.4
µM)
blast
fungus
Magnaporthe
oryzae
is
only
one‐fourth
that
isoprothiolane
(22
µM),
commercial
fungicide.
Comparative
analyzes
revealed
simultaneously
targets
conserved
Mps1
lipid
Cap20.
Surface
plasmon
resonance
assays
showed
directly
binds
to
we
provide
strategy
developing
agents
by
modifying
resultant
commercially
valuable,
eco‐friendly
broad‐spectrum
combat
disease.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(23), P. 13015 - 13022
Published: May 29, 2024
The
extensive
and
repeated
application
of
chemical
fungicides
results
in
the
rapid
development
fungicide
resistance.
Novel
antifungal
pesticides
are
urgently
required.
Natural
products
have
been
considered
precious
sources
pesticides.
It
is
necessary
to
discover
by
using
natural
products.
Herein,
42
various
griseofulvin
derivatives
were
synthesized.
Their
activities
evaluated
vitro.
Most
them
showed
good
activity,
especially
3d
exhibited
a
very
broad
spectrum
most
significant
against
7
phytopathogenic
fungi.
In
vivo
activity
suggested
that
protected
apples
tomatoes
from
serious
infection
These
proved
had
potential
be
product-derived
antiphytopathogenic
fungi
agent.
Furthermore,
docking
analysis
tubulin
might
one
action
sites
3d.
reasonable
believe
worth
further
for
discovery
new
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 20, 2024
To
develop
novel
fungicides
for
controlling
postharvest
fungal
diseases
in
citrus
fruits,
12
essential
oil
(EO)-based
thiosemicarbazones
compounds,
termed
hydrazine-carbothioamide,
were
prepared
according
to
the
condensation
method.
