Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
354(2)
Published: Oct. 12, 2020
Abstract
The
novel
compounds
with
the
chemical
structure
of
N
‐({4‐[
′‐(substituted)sulfamoyl]phenyl}carbamothioyl)benzamide
(
1a–g
)
and
4‐fluoro‐
2a
–
g
were
synthesized
as
potent
selective
human
carbonic
anhydrase
(hCA)
I
hCA
II
candidate
inhibitors.
aryl
part
was
changed
to
sulfacetamide,
sulfaguanidine,
sulfanilamide,
sulfathiazole,
sulfadiazine,
sulfamerazine,
sulfametazine.
K
i
values
1a
in
range
20.73
±
4.32
59.55
13.07
nM
(hCA
I)
5.69
0.43
44.81
1.08
II),
whereas
13.98
2.57
75.74
13.51
8.15
1.5
49.86
6.18
II).
Comparing
final
acetazolamide,
compound
1c
sulfanilamide
moiety
=
nM,
8.8
times)
2f
sulfamerazine
6.2
demonstrated
promising
inhibitory
effects
against
isoenzyme,
main
target
protein
glaucoma.
Furthermore,
1d
4.32,
4
2d
2.57,
5.9
times),
which
have
sulfathiazole
moiety,
found
Compounds
can
be
considered
lead
determined
present
study,
investigated
further
alleviate
glaucoma
symptoms.
Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
354(1)
Published: Sept. 28, 2020
Abstract
A
novel
series
of
sulfonamides,
4‐(3‐phenyltriaz‐1‐en‐1‐yl)‐
N
‐(4‐methyl‐2‐pyrimidinyl)benzenesulfonamides
(
1
–
9
),
was
designed
and
synthesized
by
the
diazo
reaction
between
sulfamerazine
substituted
aromatic
amines
for
first
time.
Their
chemical
structures
were
characterized
H
nuclear
magnetic
resonance
(NMR),
13
C
NMR,
high‐resolution
mass
spectra.
The
newly
compounds
evaluated
in
terms
acetylcholineasterase
(AChE)
human
carbonic
anhydrases
(hCA)
I
II
isoenzymes
inhibitory
activities.
According
to
AChE
inhibition
results,
K
i
values
range
19.9
±
1.5
96.5
20.7
nM
against
AChE.
Tacrine
used
as
reference
drug
its
value
49.2
2.7
10.2
2.6
101.4
27.8
hCA
I,
whereas
they
18.3
4.4
48.1
4.5
II.
Acetazolamide
a
72.2
5.4
52.2
5.7
II,
respectively.
most
active
compounds,
(nonsubstituted)
AChE,
5
(4‐ethoxy‐substituted)
8
(4‐bromo‐substituted)
chosen
docked
at
binding
sites
these
enzymes
explain
activities
series.
presented
satisfactory
pharmacokinetic
properties
via
estimation
ADME
properties.
Current Medicinal Chemistry,
Journal Year:
2022,
Volume and Issue:
30(4), P. 407 - 480
Published: June 23, 2022
Sulfonamides
constitute
an
important
class
of
drugs,
with
many
types
pharmacological
agents
possessing
antibacterial,
anti-carbonic
anhydrase,
anti-obesity,
diuretic,
hypoglycemic,
antithyroid,
antitumor,
and
anti-neuropathic
pain
activities.
The
sulfonamides
are
the
compounds
that
have
general
formula
R-SO2NHR',
where
functional
group
is
bound
to
aromatic,
heterocycle,
aliphatic
groups.
nature
R
R'
moiety
variable,
starting
hydrogen
ranging
a
variety
moieties
incorporating
organic
such
as
coumarin,
isoxazole,
tetrazole,
pyrazole,
pyrrole,
so
other
pharmaceutical
active
scaffolds
lead
considerable
range
hybrids
named
sulfonamide
hybrids.
Part
A
this
review
presents
most
recent
advances
in
designing
developing
two-component
containing
indole,
quinoline,
isoquinoline,
chalcone,
pyrazole/pyrazoline,
quinazoline,
pyrimidine,
thiazole,
benzothiazole,
pyridine
between
2015
2020.
Specifically,
authors
scientific
reports
on
synthesis
biological
activity
kind
hybrid
agent.
