Pharmaceutics,
Journal Year:
2025,
Volume and Issue:
17(2), P. 180 - 180
Published: Feb. 1, 2025
Background/Objectives:
Numerous
diseases
such
as
diabetes,
Alzheimer’s
disease,
and
cancer
have
spread
in
the
whole
world,
especially
Arab
world.
Also,
various
applications
of
Schiff-base
functionalized
nanoparticles
copper
oxide
(CuO-NPs)
therapeutic
been
discovered.
Thus,
current
research
highlights
(i)
synthesis
produced
with
a
Schiff
base
(SB)
serving
capping
agent
during
their
(ii)
assessment
vitro
biological
activities
base-synthesized
(SB-CuO-NPs)
(SB).
Methods:
SB-CuO-NPs
were
characterized
using
ultraviolet-visible
(UV-Vis)
spectroscopy,
zeta
potential,
DLS
analysis,
transmission
electron
microscope
(TEM).
It
also
focuses
on
assessing
activities,
including
antioxidant,
scavenging,
anti-diabetic,
anti-Alzheimer,
anti-arthritic,
anti-inflammatory,
cytotoxic
enzymes
inhibitory
methods
described
literature.
Results:
The
results
compared
those
SB.
demonstrated
superior
when
to
SB
from
which
they
produced.
Conclusions:
this
investigation
concluded
that
CuO-NPs,
synthesized
an
alternative
agent,
exhibited
enhanced
efficacy
relative
original
In
future,
efficiency
against
Alzheimer’s,
will
be
assessed
experimental
animals
(in
vivo).
Drug Development Research,
Journal Year:
2024,
Volume and Issue:
85(4)
Published: June 1, 2024
Abstract
A
new
series
of
quinoxaline‐sulfonamide
derivatives
3
–
12
were
synthesized
using
fragment‐based
drug
design
by
reaction
quinoxaline
sulfonyl
chloride
(QSC)
with
different
amines
and
hydrazines.
The
evaluated
for
antidiabetic
anti‐Alzheimer's
potential
against
α‐glucosidase,
α‐amylase,
acetylcholinesterase
enzymes.
These
showed
good
to
moderate
potency
α‐amylase
α‐glucosidase
inhibitory
percentages
between
24.34
±
0.01%–63.09
0.02%
28.95
0.04%–75.36
0.01%,
respectively.
Surprisingly,
bis
‐sulfonamide
derivative
4
revealed
the
most
potent
activity
75.36
0.01%
63.09
α
‐glucosidase
compared
acarbose
(IP
=
57.79
67.33
0.01%),
Moreover,
exhibited
as
a
minute
decline
from
compound
44.93
38.95
0.01%.
Additionally,
in
vitro
designed
weak
activity.
Still,
sulfonamide‐quinoxaline
emerged
active
member
percentage
41.92
donepezil
67.27
0.60%).
DFT
calculations,
docking
simulation,
target
prediction,
ADMET
analysis
performed
discussed
detail.
Pharmaceuticals,
Journal Year:
2024,
Volume and Issue:
17(5), P. 655 - 655
Published: May 17, 2024
In
this
innovative
research,
we
aim
to
reveal
pyrazole-based
Schiff
bases
as
new
multi-target
agents.
context,
re-synthesized
three
sets
of
bases,
5a–f,
6a–f,
and
7a–f,
evaluate
their
biological
applications.
The
data
from
in
vitro
assays
(including
antioxidant
scavenging
activities,
anti-diabetes,
anti-Alzheimer’s,
anti-inflammatory
properties)
the
7a–f
showed
that
six
5a,
5d,
5e,
5f,
7a,
7f
possess
highest
properties
among
compounds
evaluated.
cytotoxicity
against
lung
(A549)
colon
(Caco-2)
human
cancer
types,
well
normal
(WI-38)
cell
lines,
was
investigation
demonstrated
7a
are
active
cells,
while
two
5e
exhibited
towards
cells.
Additionally,
enzymatic
activities
caspase-3
Bcl-2
were
Furthermore,
assessed
silico
absorption,
distribution,
metabolism,
toxicity
(ADMT)
more
potent
bases.
After
modifying
structures
plan
further
extend
studies
future.
Molecules,
Journal Year:
2025,
Volume and Issue:
30(2), P. 366 - 366
Published: Jan. 17, 2025
Heterocyclic
compounds,
especially
those
containing
the
pyrazole
moiety,
are
highly
significant
in
organic
chemistry
and
possess
remarkable
diverse
biological
properties.
The
5-aminopyrazole
derivatives
key
starting
materials
for
synthesis
of
numerous
bioactive
compounds
such
as
pyrazolopyridine,
pyrazolopyrimidine,
pyrazoloquinazoline,
pyrazolotriazine
derivatives.
Many
inspired
by
a
wide
spectrum
activities
medicinal
applications
antioxidants,
anticancer
agents,
enzyme
inhibitors,
antimicrobials,
anti-tuberculosis
activities.
This
review
summarizes
recently
reported
methods
fused
pyrazole-based
based
on
within
last
5
years
(2020
to
present).
One
important
goals
this
is
illustrate
future
strategies
design,
development,
utilization
products
potent
drugs.
Pharmaceutics,
Journal Year:
2025,
Volume and Issue:
17(3), P. 293 - 293
Published: Feb. 23, 2025
Background/Objectives:
Recently,
the
prevalence
of
diseases
such
as
diabetes,
arthritis,
and
inflammatory
diseases,
along
with
their
complications,
has
become
a
significant
health
problem.
This
is
in
addition
to
various
biomedical
applications
pyrazole,
isatin,
indole
derivatives.
Accordingly,
cooperation
will
continue
between
chemistry
scientists,
pharmaceutical
human
doctors
produce
hybrid
compounds
from
pyrazole
isatin
or
possessing
biological
activities
anti-diabetic,
anti-arthritic,
anti-inflammatory
agents.
Methods:
The
two
series
pyrazole–isatin
conjugates
12a–h
pyrazole–indole
14a–d
were
prepared
our
previous
works
via
direct
reaction
5-amino-pyrazoles
10a–d
N-alkyl
11a,b,
1H-indole-3-carbaldehyde
(13),
respectively,
using
previously
reported
procedure.
potential
agents
assessed
through
estimated
inhibition
percentage
(%)
median
inhibitory
concentrations
(IC50)
methods
described
literature.
Further,
computational
assessments
toxic
doses
(the
lethal
dose,
LD50),
toxicity
classes,
drug-likeness
model
scores
(DLMS),
molecular
lipophilicity
(MLP)
maps,
polar
surface
area
(PSA)
topological
(TPSA)
values
predicted
available
free
websites.
Results:
vitro
enzymatic
assessment
results
showed
that
conjugate
14b
possesses
powerful
against
(i)
α-amylase
(%
=
65.74
±
0.23,
IC50
4.21
0.03
µg/mL)
α-glucosidase
55.49
2.76
0.01
µg/mL);
(ii)
protein
denaturation
enzyme
49.30
0.17)
proteinase
46.55
an
value
6.77
µg/mL;
(iii)
COX-1,
COX-2,
5-LOX
enzymes
5.44
0.03,
5.37
0.04,
7.52
which
almost
close
indomethacin
zileuton
drugs.
Also,
lipophilic
properties
thus
can
cross
cell
membranes,
effective
for
treatment;
all
possess
TPSA
more
than
140
Å2
good
intestinal
absorption.
Conclusions:
synthesized
works.
these
concluded
studied
results.
In
future,
research
team
present
vitro,
vivo
biological,
hopefully
obtain
effectual
anti-inflammatory.
