Synthetic Communications,
Год журнала:
2024,
Номер
unknown, С. 1 - 21
Опубликована: Ноя. 26, 2024
Thiazole
derivatives
(7a-f
and
9a-i)
were
synthesized
in
good
yields
(up
to
98%).
The
synthetic
protocol
is
achieved
through
a
two-step
reaction.
candidates
then
evaluated
for
their
antimicrobial
efficacies
against
gram-positive
gram-negative
bacteria.
4-methyl-2-(2-(3-(pentyloxy)benzylidene)hydrazinyl)-5-(p-tolyldiazenyl)thiazole
showed
significant
activity
Staphylococcus
aureus
(ATCC:
13565)
compared
ampicillin.
On
the
other
hand,
2-(2-(3-(hexyloxy)benzylidene)hydrazinyl)-4-(4-methoxyphenyl)thiazole
shows
potent
Klebsiella
pneumonia
10031)
gentamicin
as
standard
antibiotic.
ADME
profile
of
prepared
compounds
indicated
favorable
pharmacological
behaviors.
Additionally,
docking
in-silico
ADMET
analyses
performed
promising
results
revealed
strong
activity.
DFT
calculations
performed,
which
provided
additional
insight
into
thiazoles'
structure
formation.
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2024,
Номер
39(1)
Опубликована: Июнь 24, 2024
Inhibition
of
α-glucosidase
and
α-amylase
are
key
tactics
for
managing
blood
glucose
levels.
Currently,
stronger,
more
accessible
inhibitors
needed
to
treat
diabetes.
Indeno[1,2-b]
quinoxalines-carrying
thiazole
hybrids
1–17
were
created
described
using
NMR.
All
analogues
tested
hypoglycaemic
effect
against
STZ-induced
diabetes
in
mice.
Compounds
4,
6,
8,
16
the
most
potent
among
synthesised
analogues.
These
examined
their
effects
on
plasma
insulin,
urea,
creatinine,
GSH,
MDA,
ALT,
AST,
total
cholesterol.
Moreover,
these
compounds
enzymes
vitro.
The
four
represented
moderate
activity
with
IC50
values
0.982
±
0.04,
10.19
0.21
inhibition
17.58
0.74
121.6
5.14
μM
when
compared
standard
medication
acarbose
IC50=0.316
0.02
31.56
1.33
inhibition.
Docking
studies
as
well
silico
ADMT
done.
Future Medicinal Chemistry,
Год журнала:
2025,
Номер
17(3), С. 347 - 362
Опубликована: Янв. 21, 2025
The
escalating
cases
of
type
II
diabetes
combined
with
adverse
side
effects
current
antidiabetic
drugs
spurred
the
advancement
innovative
approaches
for
management
postprandial
glucose
levels.
α-Amylase
is
an
endoamylase
responsible
breakdown
internal
α-1,4-glycosidic
linkages
in
dietary
starch,
producing
oligosaccharides.
Subsequently,
α-glucosidase
degraded
these
oligosaccharides
to
monosaccharides,
which
are
absorbed
into
bloodstream
and
become
available
body.
inhibitors
α-amylase
reduced
digestibility
carbohydrates
accompanied
by
delayed
absorption,
leading
decreased
blood
levels
after
meals
thus,
inhibition
enzyme
seems
be
a
crucial
strategy
improving
overall
glycemic
control
diabetic
patients.
present
review
article
emphasizes
therapeutic
promise
recently
discovered
potential
inhibitors,
highlighting
their
vitro,
silico
vivo
profiles.
Ultimately,
we
addressed
contemporary
challenges
routes
ahead
search
safe
reliable
clinical
use,
summarizing
most
recent
research
field.
Drug Development Research,
Год журнала:
2025,
Номер
86(1)
Опубликована: Фев. 1, 2025
ABSTRACT
In
this
study,
hydrazine
clubbed
thiazole
derivatives
(
3a
–
3j
)
were
obtained
by
Hantzsch
synthesis
and
characterized
MS,
1
H
NMR,
13
C
NMR.
The
inhibitory
potentials
of
the
against
diabetes‐related
enzymes
such
as
aldose
reductase
(AR),
α‐glycosidase
(α‐GLY),
α‐amylase
(α‐AMY)
experimentally
determined,
results
supported
molecular
docking.
showed
that
displayed
varied
degree
potential
activity,
with
K
I
values
covering
following
ranges:
5.47
±
0.53
to
23.89
1.46
nM
for
AR
1.76
0.01
24.81
0.15
μM
α‐GLY,
IC
50
4.94–28.17
α‐AMY,
compared
standard
epalrestat
acarbose
:
34.53
2.52
23.53
2.72
respectively).
selective
activity
these
on
antidiabetic
may
be
important
treatment
diabetes
lead
development
alternative
new
compounds
purpose.
Scientific Reports,
Год журнала:
2025,
Номер
15(1)
Опубликована: Март 21, 2025
Increased
blood
sugar
is
a
typical
manifestation
of
Type-2
Diabetes
Mellitus
(T2DM),
metabolic
disorder
that
can
be
effectively
managed
with
the
help
α-glucosidase
inhibitors.
A
range
new
chromone
based
thiosemicarbazone
derivatives
(3a-t)
was
synthesized
and
assessed
due
to
their
ability
suppress
in
this
research.
Having
IC50
values
spanning
from
6.40
±
0.15
62.81
0.79
μM,
compounds
demonstrated
strong
inhibitory
actions.
The
compound
3
k
showed
most
effect
among
all
them,
by
an
measurement
µM.
It
concluded
through
structure–activity
relationship
(SAR)
assessment
various
substituents
on
moieties
had
significant
impact
differences
inhibition.
Molecular
docking
experiments
provide
light
important
interactions,
including
π-π
interactions
hydrogen
bridges,
between
role
carbothioamide
chromenyl
groups
ligand
attachment
critical
residues
α-glucosidase.
binding
alignment,
stability,
structural
arrangement
prepared
molecules
catalytic
pocket
were
explored
using
silico
strategies
such
as
studies,
pharmacokinetic
analysis,
molecular
dynamics
simulations.
This
investigation
directed
find
favorable
profiles
for
future
progress
potential
therapeutic
agents
type
2
diabetes.
Importantly,
when
benchmarking
against
acarbose,
lead
candidate
substantially
greater
efficacy.
