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.
Catalysis Communications,
Год журнала:
2023,
Номер
176, С. 106629 - 106629
Опубликована: Фев. 23, 2023
The
demand
for
environmental
friendly
methodologies
had
shifted
the
approach
of
scientific
community
using
easy
and
green
reaction
conditions
instead
hazardous
harsh
conditions.
One
suggested
approaches,
use
catalyst
remained
prime
choice
free
reaction.
difficulty
in
separation
homogeneous
from
product
increased
attention
chemists
heterogeneous
catalysts.
present
review
summarizes
some
recent
important
developments
catalysis
"click
reaction"
obtaining
1,2,3-triazoles
via
Cu-catalyzed
1,3-dipolar
azide-alkyne
cycloaddition
(CuAAC).
A
vast
collection
papers
is
efficiently
grouped
into
two
significant
classes
to
increase
readability
language.
Firstly,
CuAAC
reactions,
secondly,
other
metal-catalyzed
(MAAC)
reactions
are
discussed.
further
sub-classes
Cu(I)-nanoparticle
catalyzed
(Cu-NPs-AAC)
simple
Cu(I)-catalyzed
(CuAAC)
reactions.
In
most
cases,
formation
1,4-disubstituted
1,2,3-triazoles,
as
reported,
was
conveniently
presented
with
help
colored
schemes.
Green Chemistry,
Год журнала:
2024,
Номер
26(7), С. 3565 - 3594
Опубликована: Янв. 1, 2024
This
review
focuses
on
the
use
of
ionic
liquids
(ILs)
in
green
synthesis
1,2,3-triazoles
which
critically
screened,
and
summarized
two
sections
i.e.
,
from
alkynes
substrates
other
than
using
ILs
as
solvent,
catalyst
both.
Archiv der Pharmazie,
Год журнала:
2024,
Номер
357(4)
Опубликована: Янв. 21, 2024
Abstract
In
the
face
of
escalating
challenges
microbial
resistance
strains,
this
study
describes
design
and
synthesis
5‐({1‐[(1
H
‐1,2,3‐triazol‐4‐yl)methyl]‐1
‐indol‐3‐yl}methylene)thiazolidine‐2,4‐dione
derivatives,
which
have
demonstrated
significant
antimicrobial
properties.
Compared
with
minimum
inhibitory
concentrations
(MIC)
values
ciprofloxacin
on
respective
compounds
5a
,
5d
5g
5l
5m
exhibited
potent
antibacterial
activity
MIC
ranging
from
16
to
25
µM.
Almost
all
synthesized
showed
lower
compared
standards
against
vancomycin‐resistant
enterococcus
methicillin‐resistant
Staphylococcus
aureus
strains.
Additionally,
majority
remarkable
antifungal
activity,
Candida
albicans
Aspergillus
niger
as
nystatin,
griseofulvin,
fluconazole.
Furthermore,
notable
effects
Plasmodium
falciparum
strain,
having
IC
50
1.31
2.79
μM
standard
quinine
(2.71
μM).
Cytotoxicity
evaluation
5a–q
SHSY‐5Y
cells
at
up
100
μg/mL
no
adverse
effects.
Comparison
control
groups
highlights
their
noncytotoxic
characteristics.
Molecular
docking
confirmed
compound
binding
target
active
sites,
stable
protein–ligand
complexes
displaying
drug‐like
molecules.
dynamics
simulations
revealed
dynamic
stability
interactions.
Rigorous
tests
molecular
modeling
unveil
effectiveness
drug‐resistant
microbes,
providing
hope
for
new
potential
safety.
A
series
of
chalcone
derivatives
were
synthesized
and
characterized
using
UV–vis,
FT-IR,
1H
NMR,
mass
spectrometry,
followed
by
the
evaluation
their
antimicrobial
antioxidant
properties.
In
vitro
screening
against
six
bacterial
strains
(Staphylococcus
aureus,
Bacillus
subtilis,
Salmonella
typhimurium,
Escherichia
coli,
Pseudomonas
aeruginosa,
Citrobacter
freundii)
two
fungal
(Aspergillus
niger
Trichoderma
harzianum)
revealed
outstanding
antibacterial
activities,
particularly
with
compound
5b,
5d,
5e
S.
compounds
5c
5h
B.
subtilis.
Notably,
5f
5g
exhibited
significant
effects
P.
while
5b
showed
highest
antifungal
activity
T.
harzianum.
All
demonstrated
remarkable
(IC50
values
0.005
μM)
0.006
being
most
potent,
comparable
to
ascorbic
acid
0.007
μM).
silico
evaluations
confirmed
favorable
drug-likeness
pharmacokinetic
properties
for
all
analogues,
adhering
both
Lipinski's
rule
Five
Veber's
rule.
Molecular
docking
studies
potent
(5e
5h)
indicated
strong
binding
affinities
PBP-1b
receptor
in
DFT
calculations
provided
valuable
insights
into
molecular
reactivity
biological
Ligand-based
enzymatic
target
predictions
indicate
that
analogues
(5a–m)
show
potential
as
inhibitors
oxidoreductases,
kinases,
enzymes,
proteases,
or
ligands
family
GPCR.
These
findings
position
promising
candidates
therapeutic
applications
combating
infections
oxidative
stress.
ACS Omega,
Год журнала:
2023,
Номер
8(7), С. 6669 - 6678
Опубликована: Фев. 13, 2023
Cancer
is
a
progressive
disease
that
frequently
encountered
worldwide.
The
incidence
of
cancer
increasing
with
the
changing
living
conditions
around
world.
side-effect
profile
existing
drugs
and
resistance
developing
in
long-term
use
increase
need
for
novel
drugs.
In
addition,
patients
are
not
resistant
to
bacterial
fungal
infections
due
suppression
immune
system
during
treatment.
Rather
than
adding
new
antibacterial
or
antifungal
drug
current
treatment
plan,
fact
anticancer
activity
has
these
effects
(antibacterial
antifungal)
will
patient's
quality
life.
For
this
purpose,
study,
series
10
naphthalene-chalcone
derivatives
were
synthesized
their
anticancer-antibacterial-antifungal
properties
investigated.
Among
compounds,
compound
2j
showed
against
A549
cell
line
an
IC50
=
7.835
±
0.598
μM.
This
also
activity.
apoptotic
potential
was
measured
by
flow
cytometry
14.230%.
58.870%
mitochondrial
membrane
potential.
Compound
inhibited
VEGFR-2
enzyme
0.098
0.005
Molecular
docking
studies
compounds
carried
out
silico
methods
caspase-3
enzymes.
