ACS Omega,
Journal Year:
2024,
Volume and Issue:
9(42), P. 42630 - 42667
Published: Oct. 14, 2024
Heterocyclic
compounds
are
of
great
interest
in
our
daily
lives.
They
widely
distributed
nature
and
synthesized
laboratories.
Heterocycles
play
an
important
role
the
metabolism
all
living
cells,
including
vitamins
coenzyme
precursors
like
thiamine
riboflavin.
Furthermore,
heterocyclic
systems
essential
building
blocks
for
creating
innovative
materials
with
intriguing
electrical,
mechanical,
biological
properties.
Also,
more
than
85%
biologically
active
chemical
entities
comprise
a
heterocycle.
As
result,
heterocycle
synthesis
piqued
researchers'
curiosity,
recent
decades,
chemists
have
concentrated
on
nitrogen-containing
cyclic
nuclei
structures.
Quinoline
its
derivatives
exhibit
several
functions,
antimicrobial,
anticancer,
antimalarial,
anti-inflammatory,
antihypertensive,
antiasthmatic
effects.
In
addition,
over
hundred
quinoline-based
drugs
available
to
treat
variety
disorders.
Because
importance,
researchers
developed
one-pot
synthetic
methods
employing
effective
acid/base
catalysts
(Lewis
acids,
Brønsted
ionic
liquids),
reagents,
transition-metal-based
catalysts.
These
some
downsides,
longer
reaction
times,
harsher
conditions,
creation
byproducts,
costly
catalysts,
use
hazardous
solvents,
unacceptable
economic
yield,
catalyst
recovery.
Researchers'
focus
has
switched
environmentally
friendly
quinoline
as
result
these
methodologic
shortcomings.
special
qualities,
nanocatalysts
or
nanocomposites
offers
option
quinolines.
This
review
focuses
published
research
articles
synthesize
substituted
derivatives.
covers
contributions
until
May
2024,
focusing
ring
mechanistic
issues.
With
aid
this
review,
we
anticipate
that
will
be
able
develop
synthesizing
Small,
Journal Year:
2023,
Volume and Issue:
19(42)
Published: June 15, 2023
With
the
advantages
of
diverse
structures,
tunable
enzymatic
activity,
and
high
stability,
nanozymes
are
widely
used
in
medicine,
chemistry,
food,
environment,
other
fields.
As
an
alternative
to
traditional
antibiotics,
attract
more
attention
from
scientific
researchers
recent
years.
Developing
nanozymes-based
antibacterial
materials
opens
up
a
new
avenue
for
bacterial
disinfection
sterilization.
In
this
review,
classification
their
mechanisms
discussed.
The
surface
composition
critical
efficacy,
which
can
be
tailored
enhance
both
binding
activity.
On
one
hand,
modification
enables
targeting
bacteria
that
improves
performance
including
biochemical
recognition,
charge,
topography.
modulated
achieve
enhanced
single
nanozyme-mediated
synergistic
multiple
nanozymes-mediated
cascade
catalytic
applications.
addition,
current
challenges
future
prospects
tailoring
applications
This
review
provide
insights
into
design
treatments.
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2023,
Volume and Issue:
41(21), P. 11518 - 11534
Published: Jan. 24, 2023
A
class
of
2-(1H-imidazol-1-yl)-1-phenylethyl
cinnamates
6a-6j
and
2-(1H-benzo[d]imidazol-1-yl)-1-phenylethyl
7a-7j
were
synthesized,
their
synthesis
was
validated
using
various
spectroscopic
techniques
like
IR,
NMR,
Mass
spectrometry.
In
addition,
the
compounds
assessed
for
in-vitro
antibacterial
against
gram-positive
gram-negative
strains
antifungal
six
different
fungal
strains.
Compounds
6
g,
7
b,
7f,
g
exhibited
significant
activity
all
bacterial
ranging
from
MIC
=
12.5-50
µg/mL,
considerable
MFC
125-200
µg/mL.
molecular
docking
study
indicated
that
7j
could
be
lodged
in
active
pocket
inhibit
C.
albicans
Sterol
14α-demethylase
(CYP51)
protein
via
interactions,
these
studies
validate
results.
Different
parameters
100
ns
MD
simulation
are
investigated
to
evaluate
dynamic
stability
protein-ligand
complexes.
According
study,
proposed
effectively
kept
interaction
structural
integrity
within
14-demethylase.
promising
lead
searching
novel
drug-like
molecules.
Furthermore,
silico
ADME
indicates
possess
physicochemical
properties
orally
bioavailable.Communicated
by
Ramaswamy
H.
Sarma.
ACS Omega,
Journal Year:
2023,
Volume and Issue:
8(20), P. 17948 - 17965
Published: May 11, 2023
Microbial
DNA
gyrase
is
regarded
as
an
outstanding
microbial
target.
Hence,
15
new
quinoline
derivatives
(5-14)
were
designed
and
synthesized.
The
antimicrobial
activity
of
the
afforded
compounds
was
pursued
via
in
vitro
approaches.
investigated
displayed
eligible
MIC
values,
particularly
against
G-positive
Staphylococcus
aureus
species.
Consequently,
S.
supercoiling
assay
performed,
using
ciprofloxacin
a
reference
control.
Obviously,
6b
10
unveiled
IC50
values
33.64
8.45
μM,
respectively.
Alongside,
exhibited
value
3.80
μM.
Furthermore,
significant
docking
binding
score
encountered
by
compound
(-7.73
kcal/mol),
surpassing
(-7.29
kcal/mol).
Additionally,
both
revealed
high
GIT
absorption
without
passing
blood
brain
barrier.
Finally,
conducted
structure-activity
relationship
study
assured
usefulness
hydrazine
moiety
molecular
hybrid
for
either
cyclic
or
opened
form.
Antibiotics,
Journal Year:
2024,
Volume and Issue:
13(2), P. 142 - 142
Published: Feb. 1, 2024
The
synthesis
and
antiplasmodial
evaluation
of
new
hybrids
combining
the
pharmacophore
structures
artemisinin,
ciprofloxacin
or
norfloxacin,
7-chloroquinoline
are
reported
in
this
study.
first
step
for
all
syntheses
is
obtainment
key
piperazine
esters
intermediates
bearing
drugs
norfloxacin.
Using
these
platforms,
18
final
compounds
were
synthesized
through
a
multistep
procedure
with
overall
yields
ranging
between
8
20%.
All
screened
their
activity
against
chloroquine-resistant
Plasmodium
falciparum
FcB1
strain.
Compounds
20,
21,
22,
28,
an
artesunate
fragment
ciprofloxacin,
exhibited
IC50
values
range
3.5–5.4
nM
excellent
selectivity
indices.
Among
moiety
on
two
them,
23
24,
afforded
1.5
1.9
nM,
respectively.
They
also
showed
most
potent
evaluated
CQ-resistant
Dd2
strain
falciparum,
demonstrating
that
those
incorporating
potent.
Finally,
combination
either
norfloxacin
moieties
single
molecular
entity
proved
to
substantially
enhance
when
compared
administration
unconjugated
counterparts
artesunate/ciprofloxacin
artesunate/norfloxacin.