Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents
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.
Язык: Английский
Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates
Yue-Gao Hu,
Narsaiah Battini,
Bo Fang
и другие.
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
270, С. 116392 - 116392
Опубликована: Апрель 1, 2024
Язык: Английский
A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(11), С. 8932 - 8961
Опубликована: Май 30, 2024
This
study
developed
a
class
of
novel
structural
antifungal
hydrazylnaphthalimidols
(HNs)
with
multitargeting
broad-spectrum
potential
Язык: Английский
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance
Zhong‐Lin Zang,
Yi-Xin Wang,
Narsaiah Battini
и другие.
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
275, С. 116626 - 116626
Опубликована: Июнь 27, 2024
Язык: Английский
Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents
Molecules,
Год журнала:
2025,
Номер
30(2), С. 243 - 243
Опубликована: Янв. 9, 2025
The
overprescription
of
antibiotics
in
medicine
and
agriculture
has
accelerated
the
development
spread
antibiotic
resistance
bacteria,
which
severely
limits
arsenal
available
to
clinicians
for
treating
bacterial
infections.
This
work
discovered
a
new
class
heteroarylcyanovinyl
quinazolones
quinazolone
pyridiniums
surmount
increasingly
severe
resistance.
Bioactive
assays
manifested
that
highly
active
compound
19a
exhibited
strong
inhibition
against
MRSA
Escherichia
coli
with
extremely
low
MICs
0.5
μg/mL,
being
eightfold
more
than
norfloxacin
(MICs
=
4
μg/mL).
rapid
bactericidal
properties
displayed
imperceptible
trends,
negligible
hemolytic
toxicity,
effective
biofilm
inhibitory
effects.
Preliminary
explorations
on
antibacterial
mechanisms
revealed
could
cause
membrane
damage,
embed
intracellular
DNA
hinder
replication,
induce
metabolic
dysfunction.
Surprisingly,
was
found
trigger
conformational
change
PBP2a
open
site,
might
account
its
high
MRSA.
In
addition,
little
effect
molecule
production
reactive
oxygen
species
indicated
death
not
caused
by
oxidative
stress.
above
comprehensive
analyses
highlighted
large
potential
as
multitargeting
broad-spectrum
agents.
Язык: Английский
A comprehensive insight into naphthalimides as novel structural skeleton of multitargeting promising antibiotics
Future Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown, С. 1 - 16
Опубликована: Фев. 16, 2025
The
globally
growing
antimicrobial
resistance
seriously
threatens
human
health,
increasing
efforts
have
been
devoting
to
the
development
of
novel
antibiotics.
Naphthalimides
contain
a
special
skeleton
cyclic
double
imides
and
naphthalene
framework,
this
unique
structure
can
exert
multitargeting
abilities
which
are
helpful
overcome
escalating
issue
resistance.
Therefore,
research
in
connection
with
naphthalimides
as
agents
is
becoming
progressively
active.
It
has
revealed
that
structural
promising
antibiotics
could
not
only
target
DNAs
enzymes,
disturb
membrane,
produce
reactive
oxygen
species,
etc.
suggesting
actions
do
induce
resistance,
but
also
show
broad
spectrum
safety
profile
pharmacokinetic
characteristics,
implying
large
potential
new
type
via
continuous
toward
naphthalimides.
This
review
presents
discusses
rational
design
strategies,
structure-activity
relationships,
mechanisms
action,
comprehensive
view
providing
insight
for
efficient,
broad-spectrum,
low-toxic
naphthalimide
Язык: Английский
Benzo-α-pyrone-derived multitargeting actions to enhance the antibacterial performance of sulfanilamides against Escherichia coli
Bioorganic Chemistry,
Год журнала:
2025,
Номер
158, С. 108339 - 108339
Опубликована: Март 5, 2025
Язык: Английский
Anti-biofilm activity of Barleria acanthoides Vahl against Methicillin-resistant Staphylococcus aureus
S. Lourdu Pouline,
S. Murugesan,
T. Leon Stephan Raj
и другие.
Current Botany,
Год журнала:
2024,
Номер
unknown, С. 157 - 163
Опубликована: Дек. 30, 2024
Methicillin-resistant
Staphylococcu
aureus
(MRSA)
biofilms
are
notoriously
difficult
to
treat
due
their
high
resistance
antibiotics.
This
study
examines
the
antibiofilm,
antibacterial,
and
molecular
docking
potential
of
Barleria
acanthoides
ethanol
extract
against
MRSA.
A
total
18
compounds
were
identified
in
GC-MS
analysis
major
beta-asarone
(34.09%),
Neophytadiene
(15.09%)
caryophyllene
(9.65%).
The
was
very
good
at
killing
bacteria;
a
minimum
inhibitory
concentration
(MIC)
0.5
mg/mL,
it
stopped
MRSA
biofilm
formation
by
80.07%.
Molecular
studies
revealed
binding
affinities
key
regulatory
proteins
LasR
SarA,
which
essential
quorum
sensing.
These
findings
suggest
B.
as
promising
source
for
developing
new
therapeutic
agents
combat
biofilm-related
infections.
Язык: Английский