Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
354(4)
Published: Dec. 7, 2020
Abstract
New
imidazolinone‐based
benzenesulfonamides
3a–e
and
4a–e
were
synthesized
in
three
steps
their
chemical
structures
confirmed
by
1
H
NMR
(nuclear
magnetic
resonance),
13
C
NMR,
high‐resolution
mass
spectrometry.
The
used
sulfacetamide
(
3a
,
4a
),
sulfaguanidine
3b
4b
sulfanilamide
3c
4c
sulfadiazine
3d
4d
sulfamerazine
3e
sulfathiazole
4e
).
compounds
evaluated
against
carbonic
anhydrase
(CA)
acetylcholinesterase
(AChE)
enzymes
to
obtain
possible
drug
candidate/s.
lead
of
the
series
human
CA
(hCA)
I,
whereas
leads
hCA
II
terms
K
i
values.
Series
4
includes
more
effective
CAs
inhibitors
than
3
(except
having
a
nitro
group
)
3.3–4.8
times
selective
corresponding
analogues
3a–d
which
hydrogen
was
located
place
group,
considering
values
II.
Compounds
where
moiety
is
available,
AChE
inhibition
with
lowest
use
secondary
sulfonamides
modification
on
inhibition,
primary
sulfonamide
substitution
inhibitory
potency.
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2020,
Volume and Issue:
39(15), P. 5449 - 5460
Published: July 21, 2020
Sulfonamide
derivatives
exhibit
a
wide
biological
activity
and
can
function
as
potential
medical
molecules
in
the
development
of
drug.
Studies
have
reported
that
compounds
an
effect
on
many
enzymes.
In
this
study,
amine
sulfonamide
(1i-11i)
were
prepared
with
reduced
imine
(1-11)
NaBH4
methanol.
The
synthesized
fully
characterized
by
spectral
data
analytical.
acetylcholinesterase
(AChE),
glutathione
S-transferase
(GST)
α-glycosidase
(α-GLY)
enzymes
determined.
For
AChE
α-GLY,
most
powerful
inhibition
was
observed
10
10i
series
KI
value
range
2.26
±
0.45–3.57
0.97
95.73
13.67–102.45
11.72
µM,
respectively.
values
for
GST
found
22.76
1.23–49.29
4.49.
Finally,
stronger
inhibitor
lower
concentrations
attachment
functional
electronegative
groups
such
two
halogens
(-Br
-CI),
-OH
to
benzene
ring
-SO2NH2.
crystal
structures
AChE,
complex
selected
4
show
importance
moieties
binding
modes
within
receptors.Communicated
Ramaswamy
H.
Sarma
Chemistry & Biodiversity,
Journal Year:
2021,
Volume and Issue:
18(4)
Published: Feb. 23, 2021
Abstract
A
series
of
six
N
‐carbamimidoyl‐4‐(3‐substituted
phenylureido)benzenesulfonamide
derivatives
were
synthesized
by
reaction
sulfaguanidine
with
aromatic
isocyanates.
In
vitro
and
in
silico
inhibitory
effects
the
novel
ureido‐substituted
investigated
spectrophotometric
methods
for
α‐glycosidase
(α‐GLY),
acetylcholinesterase
(AChE),
butyrylcholinesterase
(BChE)
enzymes
associated
diabetes
mellitus
(DM)
Alzheimer's
disease
(AD).
‐Carbamimidoyl‐4‐{[(3,4‐dichlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide
(
2f
)
showed
AChE
BChE
effects,
K
I
values
515.98±45.03
nM
598.47±59.18
nM,
respectively,
while
‐carbamimidoyl‐4‐{[(3‐chlorophenyl)carbamoyl]amino}benzene‐1‐sulfonamide
2e
strong
α‐GLY
effect,
103.94±13.06
nM.
The
antidiabetic
compounds
are
higher
than
their
anti‐Alzheimer's
because
inhibition
effect
on
diabetic
enzyme
is
greater
esterase
enzymes.
Indeed,
metabolic
important
treatment
DM
AD.
Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
354(3)
Published: Nov. 6, 2020
Abstract
Alzheimer's
disease
(AD)
is
a
neurodegenerative
disorder
characterized
by
dementia,
memory
impairment,
cognitive
dysfunction,
and
speech
impairment.
The
utility
of
cholinergic
replacement
acetylcholinesterase
(AChE)
inhibitors
in
AD
treatment
has
been
well
documented
so
far.
Recently,
studies
have
also
evidenced
that
human
carbonic
anhydrases
(hCAs)
serve
as
an
important
target
for
treatment.
In
this
direction,
the
improvement
new
multitarget
drugs,
which
can
simultaneously
modulate
several
mechanisms
or
targets
included
pathway,
may
be
potent
strategy
to
treat
AD.
light
these
data
understanding
developing
AD‐related
AChE
hCAs
inhibitors,
study,
novel
methylene‐aminobenzoic
acid
tetrahydroisoquinolynyl‐benzoic
derivatives
(
4a
–
g
6a
)
were
designed.
synthesized
analogs
experimentally
validated
their
effects
vitro
direct
enzymatic
tests.
Also,
compounds
subjected
silico
monitoring
with
Schrödinger
Suite
software
assign
binding
affinities
potential
based
on
Glide
XP
scoring,
molecular
mechanics‐generalized
Born
surface
area
computing,
validation
docking.
results
revealed
6c
(1,3‐dimethyldihydropyrimidine‐2,4‐(1
H
,3
)‐dione‐substituted,
K
I
value
33.00
±
0.29
nM),
6e
(cyclohexanone‐substituted,
18.78
0.09
6f
(2,2‐dimethyl‐1,3‐dioxan‐4‐one‐substituted,
13.62
0.21
nM)
from
benzoic
series
most
promising
derivatives,
they
exhibited
good
multifunctional
inhibition
at
all
experimental
levels
against
hCA
I,
II,
AChE,
respectively,
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2021,
Volume and Issue:
40(22), P. 12008 - 12021
Published: Aug. 23, 2021
Aldose
reductase
(AR)
and
sorbitol
dehydrogenase
(SDH)
are
important
enzymes
of
the
polyol
pathway.
In
current
study,
inhibitory
effects
vulpinic
acid
(VA)
carnosic
(CA)
usnic
(UA)
on
purified
AR
SDH
were
determined.
These
inhibition
could
be
essential
to
prevent
diabetic
complications.
from
sheep
kidney.
Then,
VA,
CA
UA
tested
in
various
concentrations
against
these
activity
vitro.
KI
values
found
as
1.46
±
0.04,
5.13
0.25
11.71
0.27
μΜ
for
UA,
respectively,
AR.
constants
15.32
0.34,
145.60
2.17
213.40
2.64
SDH.
findings
indicate
that
useful
treatment
complications.Communicated
by
Ramaswamy
H.
Sarma
