Abstract
Novel
1‐(ethyl/methyl)‐7‐(
p
‐methoxybenzyl
amino)
and
7‐amino‐6‐fluoroquinolone‐boron
difluoride
complexes
were
synthesized,
their
biological
activity
was
studied,
comparing
the
influence
of
nature
7‐substituent
as
well
N
‐1
substituent.
The
quinolone
compounds
characterized
by
IR,
UV‐Vis,
1
H,
13
C{
H}
19
F{
NMR,
mass
spectrometry.
antiproliferative
effect
new
fluoroquinolone‐boron
in
breast
cancer
(BC)
derived
cell
lines
MCF‐7
SKBR‐3
investigated.
Compounds
9
b
a
showed
cells,
,
11
7
7b
8
similar
effects
cells.
Derivatives
with
amino
moieties
at
C‐7
an
ethyl
or
methyl
group
fluoroquinolone
ring
(
)
more
efficient
both
lines.
In
addition,
8‐nitro
to
improved
against
proliferation.
These
represent
potential
drug
candidates
for
treatment.
International Journal of Molecular Sciences,
Год журнала:
2024,
Номер
25(9), С. 4919 - 4919
Опубликована: Апрель 30, 2024
Ciprofloxacin
is
a
widely
used
antibiotic
in
the
fluoroquinolone
class.
It
acknowledged
by
various
researchers
worldwide,
and
it
has
been
documented
to
have
broad
range
of
other
pharmacological
activities,
such
as
anticancer,
antiviral,
antimalarial
etc.
Researchers
exploring
synthesis
ciprofloxacin
derivatives
with
enhanced
biological
activities
or
tailored
capability
target
specific
pathogens.
The
some
most
potent
promising
derivatives,
well
synthetic
strategies
develop
them,
are
thoroughly
reviewed
this
paper.
Modification
via
4-oxo-3-carboxylic
acid
resulted
reduced
efficacy
against
bacterial
strains.
Hybrid
molecules
containing
scaffolds
displayed
effects.
current
review
paper
provides
reported
findings
on
development
novel
ciprofloxacin-based
potency
intended
therapeutic
which
will
be
great
interest
medicinal
chemists.
Molecules,
Год журнала:
2024,
Номер
29(15), С. 3538 - 3538
Опубликована: Июль 27, 2024
Cancer
is
the
second
leading
cause
of
death
in
world
following
cardiovascular
disease.
Its
treatment,
including
radiation
therapy
and
surgical
removal
tumour,
based
on
pharmacotherapy,
which
prompts
a
constant
search
for
new
more
effective
drugs.
There
are
high
costs
associated
with
designing,
synthesising,
marketing
substances.
Drug
repositioning
an
attractive
solution.
Fluoroquinolones
make
up
group
synthetic
antibiotics
broad
spectrum
activity
bacterial
diseases.
Moreover,
those
compounds
particular
interest
to
researchers
as
result
reports
their
antiproliferative
effects
cells
most
lethal
cancers.
This
article
presents
current
progress
development
fluoroquinolone
derivatives
potential
anticancer
cytotoxic
activity,
well
structure-activity
relationships,
along
possible
directions
further
development.
Chemistry & Biodiversity,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 5, 2025
ABSTRACT
Quinolone
antibiotics
are
a
crucial
class
of
synthetic
antibacterial
agents,
widely
utilized
due
to
their
broad
spectrum
activity.
Due
the
development
antimicrobial
resistance,
potency
quinolone
drugs
decreased.
Many
conventional
methods
have
been
developed
elevate
amination
rate
and
improve
yield.
These
generally
characterized
by
prolonged
reaction
durations,
high
boiling
solvents,
harsh
conditions,
costly
reagents
excessive
heat
generation,
which
adversely
affected
therapeutic
efficacy
these
compounds.
Recently,
green
chemistry
has
focused
on
sustainable
chemistry‐dependent
analogue
synthesis
that
significantly
reduce
bacterial
infections.
include
one‐pot
synthesis,
photoredox
catalysis,
phase
transfer
ultrasonic
irradiation,
microwave‐assisted,
solvent
catalyst‐free
often
utilize
energy‐efficient,
non‐toxic
less
time‐consuming
techniques,
aligning
with
principles
safety
environmental
impact.
Researchers
continuously
explore
innovative
approaches
applying
in
reactions.
This
review
includes
comprehensive
analysis
literature
from
past
15
years
Scopus,
PubMed,
Embase
WOS
using
keywords,
such
as
chemistry,
antibacterial,
highlighting
significant
advancements
emerging
trends.
work's
importance
lies
its
extensive
overview
for
quinolones
related
heterocyclic
Furthermore,
provide
useful
information
generation
future
drugs,
some
structural–activity
relationship
studies
silico
also
included
investigate
stable
binding
interactions
between
leads
various
target
proteins.
Journal of Chemical Information and Modeling,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 12, 2025
The
recent
outbreak
of
the
coronavirus
(COVID-19)
pandemic,
caused
by
SARS-CoV-2
virus,
has
posed
serious
threats
to
global
health
systems.
Although
several
directions
have
been
put
WHO
for
effective
treatment,
use
antibiotics,
particularly
ciprofloxacin,
in
suspected
and
acquired
Covid-19
patients
raised
an
even
more
concern
antibiotic
resistance.
Ciprofloxacin
reported
inhibit
entry
into
host
cells
via
interacting
with
spike
(S)
protein.
However,
a
proper
structure-activity
relationship
study
ciprofloxacin
S-protein
is
lacking,
which
inhibits
researchers
from
developing
potent
fluoroquinolone
analogue,
specific
inhibition
viral
entry.
Herein,
order
study,
we
accomplished
short
convergent
synthesis
different
derivatives
detailed
International Journal of Applied Pharmaceutics,
Год журнала:
2025,
Номер
unknown, С. 153 - 164
Опубликована: Март 7, 2025
Objective:
This
research
was
conducted
to
design
hybrid
molecules
of
FDA-approved
drugs
as
potential
inhibitors
SARS
Co-V-2
(Mpr)
using
computational
approach.
Methods:
work
focused
on
the
significance
or
Mutual
Pro-drugs.
We
have
designed
a
set
20
and
applied
Molecular
Docking,
Absorption,
Distribution,
Metabolism,
Excretion,
Toxicity
(ADMET)
tests
filter
them.
The
most
effective
molecule
then
studied
for
its
stability
Dynamic
(MD)
simulations.
Results:
found
that
PH-6a
has
very
low
binding
energy
of-7.58kcal/mol
it
forms
five
hydrogen
bonds
(Met49,
Phe140,
His163,
Glu166)
pi
bond
(Cys145)
with
crucial
residues
targeted
Mpr
protein.
It
possesses
lower
toxicity,
is
impermeable
blood-brain
barrier
(BBB),
favourable
synthetic
availability
drug
scores.
Root
mean
Square
Deviation
(RMSD)
lead
compound
(PH-6a)
within
acceptable
range
3
Å
total
determined
be-5.06
kcal/mol,
indicating
higher
level
in
structure.
Conclusion:
Our
findings
offer
valuable
insights
into
their
application
development
strategies
addressing
various
emergency
viral
infections.
Additionally,
our
results
contribute
creation
library
compounds
therapeutic
properties.
