A comprehensive insight into naphthalimides as novel structural skeleton of multitargeting promising antibiotics
Langming Mou,
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WU Xian-hua,
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Aisha Bibi
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et al.
Future Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1 - 16
Published: Feb. 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
Language: Английский
Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents
Yi-Min Tan,
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Jing Zhang,
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Yu-Jia Wei
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et al.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(11), P. 9028 - 9053
Published: May 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.
Language: Английский
A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates
Jin‐Xing Wang,
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Pengli Zhang,
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Lavanya Gopala
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et al.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(11), P. 8932 - 8961
Published: May 30, 2024
This
study
developed
a
class
of
novel
structural
antifungal
hydrazylnaphthalimidols
(HNs)
with
multitargeting
broad-spectrum
potential
Language: Английский
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance
Zhong‐Lin Zang,
No information about this author
Yi-Xin Wang,
No information about this author
Narsaiah Battini
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et al.
European Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
275, P. 116626 - 116626
Published: June 27, 2024
Language: Английский
Discovery of Quinazolone Pyridiniums as Potential Broad-Spectrum Antibacterial Agents
Jie Dai,
No information about this author
Qianyue Li,
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Ziyi Li
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et al.
Molecules,
Journal Year:
2025,
Volume and Issue:
30(2), P. 243 - 243
Published: Jan. 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.
Language: Английский
Benzo-α-pyrone-derived multitargeting actions to enhance the antibacterial performance of sulfanilamides against Escherichia coli
Yixin Wang,
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Haoran Wang,
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Jiang-Sheng Zhao
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et al.
Bioorganic Chemistry,
Journal Year:
2025,
Volume and Issue:
158, P. 108339 - 108339
Published: March 5, 2025
Language: Английский
Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates
Yue-Gao Hu,
No information about this author
Narsaiah Battini,
No information about this author
Bo Fang
No information about this author
et al.
European Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
270, P. 116392 - 116392
Published: April 1, 2024
Language: Английский
Identification of hydroxyphenyl cyanovinyl thiazoles as new structural scaffold of potential antibacterial agents
Lu Xing,
No information about this author
Shaolin Zhang,
No information about this author
Cheng‐He Zhou
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et al.
Bioorganic & Medicinal Chemistry Letters,
Journal Year:
2025,
Volume and Issue:
unknown, P. 130258 - 130258
Published: April 1, 2025
Language: Английский
Natural Coumarin‐Hybridized Thiazolylbenzonitriles as New Structural Scaffolds to Exert Potentially Multitargeting Supramolecular Antibacterial Behavior
Qianyue Li,
No information about this author
Chun‐Mei Zeng,
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Qianming Chen
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et al.
Chinese Journal of Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: May 20, 2025
Comprehensive
Summary
A
unique
type
of
natural
coumarin
skeleton‐based
thiazolylbenzonitriles
as
novel
structural
scaffolds
to
exert
potential
multitargeting
supramolecular
antibacterial
behavior
was
developed
for
the
first
time
from
resorcinol
through
multi‐step
reactions.
All
new
compounds
were
characterized
by
NMR
and
HRMS
spectra.
Structure‐activity
relationships
revealed
that
ethoxycarbonyl
group
optimal
substituent
effective
action
benzopyronyl
(BTBs),
BTB
13a
gave
an
extremely
low
MIC
value
0.002
mM
against
Staphylococcus
aureus
29213,
being
3‐fold
more
active
than
norfloxacin.
Compound
exerting
most
behaviour
possessed
favourable
druggability
with
no
obvious
haemolysis,
acceptable
cytotoxicity
propensity
induce
bacterial
resistance.
series
medicinal
chemobiological
evaluations
disclosed
could
not
only
intercalate
into
DNA
produce
stable
biosupramolecular
complexes
block
replication,
form
biosupermolecules
gyrase,
but
also
disturb
cell
membrane
tempt
leakage
intracellular
contents,
fluctuate
metabolism
oxidative
stress,
finally
resulting
in
death.
Moreover,
promising
exhibited
good
vivo
efficacy
29213.
These
results
implied
large
promise
members
combat
Language: Английский
Anti-biofilm activity of Barleria acanthoides Vahl against Methicillin-resistant Staphylococcus aureus
S. Lourdu Pouline,
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S. Murugesan,
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T. Leon Stephan Raj
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et al.
Current Botany,
Journal Year:
2024,
Volume and Issue:
unknown, P. 157 - 163
Published: Dec. 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.
Language: Английский