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
Novel coumarin-thiazolidine-2,4-dione hybrids as potential α-glucosidase inhibitors: Synthesis and bioactivity evaluation
Journal of Molecular Structure,
Год журнала:
2024,
Номер
unknown, С. 140481 - 140481
Опубликована: Окт. 1, 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
In silico screening and synthesis of stable tilmicosin-hydrazone derivatives as potential DNA disruptors towards Staphylococcus aureus
Bioorganic Chemistry,
Год журнала:
2025,
Номер
158, С. 108336 - 108336
Опубликована: Март 5, 2025
Язык: Английский
Investigation of recent advancement in the pharmacological potential of C-3 substituted coumarin derivatives against S. aureus
P. K. Tandel,
Zebabanu Khalifa,
Rachana Upadhyay
и другие.
Discover Chemistry.,
Год журнала:
2025,
Номер
2(1)
Опубликована: Март 26, 2025
In
recent
years,
microbial
infections
have
become
the
most
common
and
leading
cause
of
death
worldwide.
From
them,
Gram-positive
bacterial
strain
Staphylococcus
aureus
is
a
highly
effective
pathogen
that
can
infect
almost
every
human
body
tissue,
from
minor
skin
diseases
to
life-threatening
infections.
Antibiotics
are
generally
used
treat
infections,
but
due
their
excessive
careless
usage,
microorganisms
gradually
developed
resistance
them.
Therefore,
it
necessary
develop
novel
drugs
minimize
drug
resistance.
Many
available
in
market
they
not
as
before.
Currently,
coumarin
derivatives
regarded
medicinal
chemistry
favored
by
new
researchers
diverse
pharmaceutical
properties,
including
antibacterial,
anticancer,
antitubercular,
antioxidant,
etc.
It
also
possesses
antibiotic
qualities
well.
Coumarines
commercially
long
been
utilized
clinical
treatment.
These
therapeutic
properties
help
antimicrobial
agents
Hence,
this
review
article
provides
significant
attention
developments
structure–activity
relationships
(SAR)
C-3
substituted
combat
infection
caused
S.
aureus.
Язык: Английский