RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(2), P. 1018 - 1033
Published: Jan. 1, 2024
IC
50
values
of
the
new
synthesized
pyrazoline-acyl
thioureas
revealed
5b
and
5g
as
potent
urease
inhibitors.
Whilst
compound
is
a
α-glucosidase
inhibitor,
5f
amylase
antioxidant.
Chemistry,
Journal Year:
2024,
Volume and Issue:
6(3), P. 435 - 468
Published: May 31, 2024
Thiourea
and
its
derivatives
have
become
a
significant
focal
point
within
the
organic
synthesis
field,
garnering
attention
for
their
diverse
biological
applications,
including
antibacterial,
antioxidant,
anticancer,
anti-inflammatory,
anti-Alzheimer,
antituberculosis
antimalarial
properties.
My
objective
is
to
present
comprehensive
easily
understandable
analysis
of
recent
advancements
in
thiourea
derivatives.
focus
on
structure
activity
these
over
past
five
years,
highlighting
progress
made
field
synthesis.
Additionally,
I
evaluate
current
state
research
this
area
provide
an
overview
latest
trends
future
prospects.
This
review
will
prove
be
beneficial
researchers,
academics
industry
professionals
involved
drug
development
RSC Advances,
Journal Year:
2023,
Volume and Issue:
13(36), P. 24988 - 25001
Published: Jan. 1, 2023
A
series
of
ten
novel
compounds
were
synthesized
by
incorporating
a
1,3
thiazole
core
into
amantadine
and
their
structures
validated
using
different
analytical
spectral
methods
such
as
FTIR,
EI-MS,
1H
NMR,
13C
NMR.
The
antibacterial
enzyme
inhibitory
properties
these
newly
evaluated.
Remarkably,
the
exhibited
significant
activity
against
Escherichia
coli
Bacillus
subtilis.
Additionally,
in
vitro
activities
compounds,
α-amylase,
α-glucosidase,
urease
investigated.
Among
tested
compound
6d
demonstrated
potent
selective
inhibition
α-amylase
IC50
=
97.37
±
1.52
μM,
while
acarbose
was
used
positive
control
5.17
0.25
μM.
Compound
6e
prominent
α-glucosidase
38.73
0.80
μM
41.63
0.26
respectively.
Furthermore,
inhibited
with
exceptional
efficacy
32.76
thiourea
showed
more
having
1.334
Molecular
docking
studies
disclosed
binding
mechanism
affinity
new
inhibitors
within
sites
various
amino
acids.
To
investigate
association
between
molecular
structural
characteristics
actions
derivatives,
preliminary
structure-activity
relationship
(SAR)
performed.
These
findings
indicated
that
6a,
6c,
are
potential
candidates
for
hit-to-lead
follow-up
drug-discovery
process
treating
diabetes
hyperglycemia.
