Abstract
Alpha
‐amylase
plays
a
crucial
role
in
blood
glucose
levels,
and
thus,
its
inhibitor
can
be
used
to
control
diabetes.
Thus,
vitro
alpha
inhibitory
activities
were
studied
for
synthesized
benzoxazole
compounds.
The
2‐amino‐benzoxazoles
prepared
by
reacting
2‐aminophenol
with
cyanogen
bromide,
which
was
coupled
phenoxy
acetic
acid
derivatives
(
6
a‐n
).
compound
h
found
significantly
active
IC
50
values
of
348.43
μg/mL
against
compared
acarbose
(IC
=682.54
μg/mL).
molecular
docking
dynamic
simulation
showed
better
affinity
stability
at
the
binding
site
protein.
Further,
preliminary
bioevalauation
antidiabetic
study
done
through
vivo
using
SD
rats.
efficacy
significant
improvement
total
cholesterol,
triglyceride,
LDL,
HDL
levels
lead
agent.
Antibiotics,
Год журнала:
2023,
Номер
12(7), С. 1220 - 1220
Опубликована: Июль 22, 2023
Bacterial
infections
have
attracted
the
attention
of
researchers
in
recent
decades,
especially
due
to
special
problems
they
faced,
such
as
their
increasing
diversity
and
resistance
antibiotic
treatment.
The
emergence
development
SARS-CoV-2
infection
stimulated
even
more
research
find
new
structures
with
antimicrobial
antiviral
properties.
Among
heterocyclic
compounds
remarkable
therapeutic
properties,
benzimidazoles,
triazoles
stand
out,
possessing
antimicrobial,
antiviral,
antitumor,
anti-Alzheimer,
anti-inflammatory,
analgesic,
antidiabetic,
or
anti-ulcer
activities.
In
addition,
literature
last
decade
reports
benzimidazole-triazole
hybrids
improved
biological
properties
compared
simple
mono-heterocyclic
compounds.
This
review
aims
provide
an
update
on
synthesis
methods
these
hybrids,
along
activities,
well
structure-activity
relationship
reported
literature.
It
was
found
that
presence
certain
groups
grafted
onto
benzimidazole
and/or
triazole
nuclei
(-F,
-Cl,
-Br,
-CF3,
-NO2,
-CN,
-CHO,
-OH,
OCH3,
COOCH3),
some
heterocycles
(pyridine,
pyrimidine,
thiazole,
indole,
isoxazole,
thiadiazole,
coumarin)
increases
activity
hybrids.
Also,
oxygen
sulfur
atom
bridge
connecting
rings
generally
mentions
only
benzimidazole-1,2,3-triazole
Both
for
additional
ring
activity,
which
is
agreement
three-dimensional
binding
mode
summarizes
advances
derivatives
potential
agents
covering
articles
published
from
2000
2023.
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.
Marine Drugs,
Год журнала:
2025,
Номер
23(4), С. 159 - 159
Опубликована: Апрель 4, 2025
α-Amylases,
catalyzing
starch
degradation,
serve
as
vital
biocatalysts
in
industrial
and
pharmaceutical
applications.
This
study
identified
a
new
α-amylase,
Alphaz,
from
Nocardiopsis
aegyptia
HDN19-252
of
Antarctic
animal
origin,
achieving
heterologous
expression
Escherichia
coli.
Phylogenetic
analysis
confirmed
its
classification
into
the
GH13_5
subfamily
glycoside
hydrolases.
Recombinant
Alphaz
exhibited
optimal
activity
at
40
°C/pH
8.0
while
maintaining
stability
across
0–30
°C
pH
6.6–9.6.
Its
distinctive
halotolerant
properties
included
full
retention
0.6
M
NaCl
>60%
efficiency
salt-free
conditions.
The
enzyme
exhibits
tolerance
to
K+,
Ca2+,
Fe³+
demonstrating
specific
inhibition
by
Cu2+/Zn2+.
With
heterologously
validated
functional
properties,
emerges
programmable
enzymatic
tool
offering
advantages
sustained-release
formulation
quality
control,
targeted
prodrug
modification,
precision
medicine
applications,
thereby
enabling
sustainable
biomanufacturing
solutions
that
harmonize
process
reliability
with
environmental
compatibility.
