Zeitschrift für Naturforschung C,
Год журнала:
2024,
Номер
unknown
Опубликована: Ноя. 20, 2024
Abstract
Diabetes
mellitus
(DM)
is
a
disorder
which
raised
at
the
alarming
level
and
it
characterized
by
hyperglycemia
results
from
impaired
action
of
insulin,
production
insulin
or
both
these
simultaneously.
Consequently,
causes
problems
failure
different
body
organs
such
as
kidneys,
heart,
eyes,
nerve
system.
Since
this
disease
cannot
be
completely
cured
until
now,
we
aimed
to
design
series
enzymes
inhibitors
tested
them
for
DM
treatment.
In
series,
benzimidazole-based
thiazolidinone
bearing
chalcone
derivatives
completed
in
four
step
reaction
their
structures
were
confirmed
through
various
spectroscopic
techniques.
A
significant
efficacy
on
antidiabetic
was
observed,
with
IC
50
values
ranging
25.05
±
0.04
56.08
0.07
μM
α-amylase
22.07
0.02
53.06
α-glucosidase.
The
obtained
compared
those
standard
glimepiride
drug
(IC
=
18.05
µM
15.02
0
.03
α-glucosidase).
synthesized
compounds
showed
promising
potency.
Moreover,
molecular
docking
study
conducted
most
active
analogs
better
understand
interactions
sites
targeted
enzymes.
Abstract
A
ring
annelation
reaction
was
used
to
successfully
prepare
benzo[4,5]imidazo[1,2-
a
][1,3,5]triazines
(Systematic
Name:
1,3,4a,9-tetraza-4
H
-fluoren-2-amines)
tethered
phenoxy-
N
-arylacetamide,
pyrazole,
and
2-(4-(1-phenyl-1
-pyrazol-3-yl)phenoxy)-
-arylacetamide
moieties
utilizing
1-(1
-benzo[
d
]imidazol-2-yl)guanidine
the
proper
aldehydes
as
precursors.
2-(Phenylamino)ethyl
fragment
of
compound
7
cleaved
off
8
formed.
The
constitutions
novel
compounds
were
confirmed
based
on
spectral
data.
antibacterial
activity
evaluated
for
prepared
against
two
gram-negative
gram-positive
bacteria.
Among
them,
12b
(inhibition
zone
16
±
0.7
mm)
most
promising
S.
aureus
compared
Gentamycin
(15
0
mm).
Also,
5a
5d
exerted
comparable
zones
13
1.4
2.1
mm),
respectively
.
Minimum
inhibitory
concentration
(MIC)
evaluation
showed
that
had
lowest
MIC
value
(78.1
µg/mL).
Asian Journal of Organic Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 3, 2025
Abstract
A
facile
metal‐free
approach
to
5‐(1,2,3‐triazol‐1‐yl)isoxazoles
bearing
a
variety
of
functional
groups
in
both
heterocyles
has
been
developed.
cyclization
3‐EWG‐5‐azidoisoxazoles
with
compounds
possessing
active
methylene
group
proceeds
smoothly
under
mild
conditions
the
presence
triethylamine
or
Cs
2
CO
3
alcohols
DMF
affording
fused
hybrid
triazole‐isoxazole
high
yields
up
98%.
Some
mechanistic
aspects
reaction
are
discussed.
Abstract
This
study
reports
the
synthesis
and
biological
evaluation
of
two
series
novel
hybrid
heterocyclic
scaffolds
tethering
1,2,3‐triazole
benzimidazole
moieties
using
click
chemistry
approach.
Aromatic
azides
were
synthesized
from
aniline
derivatives
followed
by
preparation
S‐propargylated
intermediates.
These
intermediates
then
reacted
with
through
1,3‐dipolar
cycloaddition
to
yield
benzimidazole‐1,2,3‐triazole
hybrids.
The
compounds
fully
characterized
NMR
spectroscopy.
Biological
testing
revealed
significant
antibacterial,
antifungal,
cytotoxic
activities.
Notably,
acetamide‐linked
1,2,3‐triazole‐benzimidazole
hybrids
exhibited
potent
activity
against
Gram‐negative
bacteria
fungal
strains
MIC
values
0.156–0.312
mg/mL
several
demonstrating
selectivity
cancer
cell
lines,
particularly
HepG‐2
A‐549
IC
50
7–30
µg/mL.
EGFR‐TK
enzyme
inhibition
assays
further
highlighted
potential
these
as
anticancer
agents.
Docking
simulation
was
done
for
most
active
5d
9f
promising
triazole
hits
different
linker
structures
interaction
analogs
both
valuable
targets
contributing
growth
such
as;
EGFRWT
EGFRT790
in
disease;
fragments
contributions
are
able
stabilize
molecular
interactions.
bioactivity
positions
them
candidates
optimization
development
broad‐spectrum
antimicrobial
