Chinese Journal of Chemistry,
Год журнала:
2023,
Номер
41(24), С. 3645 - 3661
Опубликована: Авг. 28, 2023
Comprehensive
Summary
Alkaloids
are
one
of
the
prominent
members
in
development
new
antimicrobial
agents.
This
work
discovered
a
class
alkaloid
quinazolone‐derived
imidazolenones
as
novel
structural
type
antibacterial
agents
with
large
potential
to
treat
severe
bacterial
infections
agricultural
and
food
field.
Preliminary
bioactive
assay
displayed
that
some
prepared
compounds
exhibited
good
inhibition
against
tested
strains,
cyclohexylimidazole‐derived
7‐fluoroquinazolone
22a
(MIC
=
0.002
mmol/L)
12.5‐fold
stronger
than
norfloxacin
Escherichia
coli
ATCC
25922.
Further
studies
revealed
compound
not
only
possessed
ability
rapid
bactericidal
property
low
propensity
develop
resistance
but
also
showed
cytotoxic
effects
toward
red
blood
cells.
The
preliminary
mechanism
exploration
indicated
could
cause
membrane
damage
by
disrupting
well
depolarizing
cell
membrane.
Moreover,
insert
into
DNA,
which
might
hinder
replication
DNA.
Molecular
docking
suggested
bind
gyrase
topoisomerase,
be
due
suppressed
expression
related
genes.
Meanwhile,
disorder
metabolism
stimulate
production
reactive
oxygen
species
affect
growth.
series
investigations
promise
multitargeting
candidates
for
treatment
infections.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(11), С. 9028 - 9053
Опубликована: Май 24, 2024
This
work
identified
a
class
of
cyanomethylquinolones
(CQs)
and
their
carboxyl
analogues
as
potential
multitargeting
antibacterial
candidates.
Most
the
prepared
compounds
showed
high
activities
against
most
tested
bacteria,
exhibiting
lower
MIC
values
(0.125–2
μg/mL)
than
those
clinical
norfloxacin,
ciprofloxacin,
clinafloxacin.
The
low
hemolysis,
drug
resistance,
cytotoxicity,
well
good
predictive
pharmacokinetics
active
CQs
revealed
development
potential.
Furthermore,
they
could
eradicate
established
biofilm,
facilitating
bacterial
exposure
to
these
These
induce
death
through
effects,
including
intercalating
into
DNA,
up-regulating
reactive
oxygen
species,
damaging
membranes
directly,
impeding
metabolism.
Moreover,
highly
cyclopropyl
CQ
15
exhibited
more
effective
in
vivo
anti-MRSA
potency
ciprofloxacin.
findings
highlight
broad-spectrum
candidates
for
treating
intractable
infections.
Chinese Journal of Chemistry,
Год журнала:
2024,
Номер
42(15), С. 1741 - 1758
Опубликована: Март 26, 2024
Comprehensive
Summary
A
type
of
unique
azole‐hybridized
acylhydrazonyl
aloe
emodins
(AAEs)
were
developed
as
new
antibacterial
agents
for
combating
bacterial
infections.
Some
target
AAEs
showed
strong
activities,
especially,
tetrazolylthioether
AAE
27a
exhibited
broad
spectrum
with
16—256
folds
and
8—64
more
active
efficacy
than
the
reference
drugs
emodin
norfloxacin,
respectively.
Tetrazolylthioether
also
gave
low
hemolysis
cytotoxicity,
well
favorable
bioavailability.
Preliminary
mechanism
explorations
revealed
that
could
cause
membrane
depolarization
damage
cell
membrane,
resulting
in
nucleic
acid
leakage.
Moreover,
compound
intercalate
into
DNA
to
impede
its
replication
form
supramolecular
‐DNA
gyrase
complex
disturb
function
gyrase.
These
findings
would
provide
valuable
insights
further
exploration
azolyl
potential
candidates.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Янв. 6, 2025
Abstract
In
a
quest
to
innovate
biologically
active
molecules,
the
benzoylation
of
4,6-dimethylpyrimidine-2-thiol
hydrochloride
(
1
)
with
benzoyl
chloride
derivatives
was
employed
produce
series
pyrimidine
benzothioate
2–5
).
Subsequent
sulfoxidation
these
using
hydrogen
peroxide
and
glacial
acetic
acid
yielded
diverse
array
sulfonyl
methanone
6–9
parallel,
sulfonothioates
10–12
pyrimidines
13–15
),
originating
from
condensation
compound
derivatives.
The
newly
synthesized
compounds
underwent
characterization
via
FT-IR,
NMR,
mass
spectrometry,
elemental
analyses.
Biological
screenings
unveiled
interesting
properties:
6
exhibited
significant
antimicrobial
potency
against
S.
epidermidis
haemolyticus
,
whereas
11
showed
distinct
insensitivity.
Excitingly,
12
showcased
robust
antioxidant
activity
by
efficiently
scavenging
DPPH
•
radical,
underscoring
their
potential
in
oxidative
stress
mitigation.
Notably,
10
displayed
promising
anti-tumor
effects,
demonstrating
superior
efficacy
MCF-7
breast
cancer
cell
line
compared
.
study
revealed
spectrum
biological
activities
across
derivatives,
modifications
often
resulting
diminished
bioactivity
parent
These
findings
shed
light
on
intricate
relationship
between
chemical
properties,
offering
valuable
insights
for
future
drug
discovery
endeavors.
