Foods,
Journal Year:
2024,
Volume and Issue:
13(24), P. 4103 - 4103
Published: Dec. 18, 2024
The
increase
in
the
incidence
of
hyperglycemia
and
diabetes
poses
challenge
finding
cost-effective
natural
inhibitors
starch
digestion
enzymes.
Among
compounds,
phenolics
have
been
considered
as
promising
candidates.
aims
this
study
were
follows:
(a)
to
investigate
effectiveness
inhibition
different
winemaking
byproducts
towards
intestinal
brush
border
α-glucosidase
pancreatic
α-amylase
vitro;
(b)
calculate
an
efficacy
index
relative
standard
acarbose
for
phenolic
pool
byproducts,
well
isolated
compounds
pools
plants
studied
literature,
order
rank
with
respect
reference
drug
other
alternatives.
red
grape
skins
showed
highest
inhibitory
activities
both
α-amylase,
which
were,
on
average,
4.9
2.6
µg
equivalents/µg
total
(µg
Ac
eq/µg
GAE),
respectively.
A
correlation
was
observed
between
contents
their
effectiveness,
is
useful
standardizing
extracts
obtained
from
processes.
In
general,
activity
higher
than
those
namely
anthocyanins
monomeric
polymeric
flavanols
flavonols,
probably
due
synergistic
effects
among
compounds.
Hence,
bioactive
fractions
could
be
produced
focus
functionality
rather
purity,
line
principles
sustainable
processing.
Based
developed
compare
phenolic-rich
literature
enzyme
inhibitors,
proved
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.
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2024,
Volume and Issue:
unknown, P. 1 - 21
Published: March 3, 2024
In
the
current
study,
metronidazole
derivatives
containing
1H-1,2,3-triazole
and
carboxylate
moieties
were
evaluated
in
vitro
by
computational
methods
for
their
anti-diabetic
potential
to
insight
into
medicinal
use
management
of
type
II
diabetes
mellitus.
Interestingly
all
14
compounds
displayed
high
significant
inhibitory
capability
against
key
carbohydrate's
digestive
enzyme
α-glucosidase
with
IC50
values
range
9.73–56.39
μM,
as
compared
marketed
drug
acarbose
(IC50
=
873.34
±
1.67
μM).
Compounds
5i
7c
exhibited
highest
inhibition,
therefore,
these
two
further
mechanistic
studies
explore
its
inhibition.
both
a
concentration-dependent
(competitive
inhibition)
Ki
7.14
0.01,
6.15
0.02
respectively,
which
conclude
favourable
interactions
active
site
residues
α-glucosidase.
are
non-cytotoxic
BJ
cell
line.
To
validate
our
findings,
in-silico
approaches
like
molecular
docking,
dynamic
simulations
applied
investigate
mode
bindings
identifies
inhibition
mechanism,
strongly
complements
experimental
findings.
Current Topics in Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
24(18), P. 1557 - 1588
Published: May 20, 2024
Molecular
hybridization
is
a
rational
design
strategy
used
to
create
new
ligands
or
prototypes
by
identifying
and
combining
specific
pharmacophoric
subunits
from
the
molecular
structures
of
two
more
known
bioactive
derivatives.
valuable
technique
in
drug
discovery,
enabling
modulation
unwanted
side
effects
creation
potential
dual-acting
drugs
that
combine
multiple
therapeutic
agents.
Indole-triazole
conjugates
have
emerged
as
promising
candidates
for
development.
The
indole
triazole
moieties
can
be
linked
through
various
synthetic
strategies,
such
click
chemistry
other
coupling
reactions,
generate
library
diverse
compounds
biological
screening.
achievable
structural
diversity
with
indole-triazole
offers
avenues
optimize
their
pharmacokinetic
pharmacodynamic
attributes,
amplifying
efficacy.
Researchers
extensively
tailored
both
frameworks
modifications
comprehend
impact
on
drug's
characteristics.
current
review
article
endeavours
explore
discuss
research
strategies
indoletriazole
hybrids
elucidate
significance
variety
pathological
conditions.
insights
provided
herein
are
anticipated
beneficial
researchers
will
likely
encourage
further
exploration
this
field.
Future Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown, P. 1 - 21
Published: Sept. 12, 2024
By
keeping
in
aspects,
the
pharmacological
potential
of
heterocyclic
compounds,
pyrimidine-based
compounds
were
designed,
synthesized
and
evaluated
for
α-amylase
inhibitory
potential.
