Abstract
Research
has
placed
a
great
deal
of
emphasis
on
molecule
development
and
discovery
with
substantial
biological
profiling
in
recent
years.
Despite
the
significant
side
effects,
medicinal
chemists
have
long
strived
to
synthesize
drug
molecules
highest
level
therapeutic
activity
lowest
possible
toxicity.
The
naphthyl‐based
chalcone
derivatives
drawn
attention
due
their
simple
structures
wide
range
pharmacological
effects.
main
focus
this
review
is
outline
biologically
active
based
naphthyl
moiety‐substituted
developed
over
A
synopsis
screening,
including
relevant
structure‐activity
relationships,
action
mechanisms,
applications,
provided
article.
It
true
that
prospective
hybrids
combining
moiety
different
pharmacophores
are
needed
address
resistance
improve
specificity.
Therefore,
may
be
useful
design
new,
highly
successful
drugs
previously
reported
methodologies.
ACS Omega,
Год журнала:
2022,
Номер
8(1), С. 1410 - 1429
Опубликована: Дек. 29, 2022
Infectious
diseases
are
a
major
concern
around
the
world.
Today,
it
is
an
urgent
need
for
new
chemotherapeutics
infectious
diseases.
Because
of
that,
our
group
designed,
synthesized,
and
analyzed
14
quinoline
derivatives
endowed
with
pharmacophore
moiety
fluoroquinolones
primarily
their
antimicrobial
effects.
Their
cytotoxicity
effects
were
tested
against
six
bacterial
four
fungal
strains
NIH/3T3
cell
line.
Additionally,
action
mechanisms
evaluated
DNA
gyrase
lanosterol
14α-demethylase
(LMD).
Furthermore,
to
eliminate
potential
side
effects,
active
compounds
aromatase
enzyme.
The
experimental
enzymatic
results
compounds'
binding
modes
using
molecular
docking
dynamics
simulation
studies.
utilized
clarify
structure–activity
relationship
(SAR).
Finally,
compound
4m
was
most
potent
its
antifungal
activity
low
healthy
cells
fewer
possible
while
4j
4l
can
be
used
alone
special
patients
who
suffering
from
infections
in
addition
primer
disease.
Abstract
Research
has
placed
a
great
deal
of
emphasis
on
molecule
development
and
discovery
with
substantial
biological
profiling
in
recent
years.
Despite
the
significant
side
effects,
medicinal
chemists
have
long
strived
to
synthesize
drug
molecules
highest
level
therapeutic
activity
lowest
possible
toxicity.
The
naphthyl‐based
chalcone
derivatives
drawn
attention
due
their
simple
structures
wide
range
pharmacological
effects.
main
focus
this
review
is
outline
biologically
active
based
naphthyl
moiety‐substituted
developed
over
A
synopsis
screening,
including
relevant
structure‐activity
relationships,
action
mechanisms,
applications,
provided
article.
It
true
that
prospective
hybrids
combining
moiety
different
pharmacophores
are
needed
address
resistance
improve
specificity.
Therefore,
may
be
useful
design
new,
highly
successful
drugs
previously
reported
methodologies.
