Abstract
Enzyme
inhibition
is
a
frequently
employed
technique
for
regulating
enzyme
activity
in
several
biological
systems
that
are
physiologically
significant.
In
this
study,
it
was
evaluated
the
effectiveness
of
six
specific
quinolone
medicines,
namely
lomefloxacin,
nalidixic
acid,
gatifloxacin,
norfloxacin,
sparfloxacin
and
nitrofurantoin,
inhibiting
two
human
isoforms
carbonic
anhydrase
(hCA)
play
role
different
physiological
pathological
circumstances.
order
to
achieve
objective,
both
vitro
silico
investigations
were
conducted
get
deeper
understanding
potential
binding
interactions
affinities
hCA
I
II
isoforms.
The
kinetic
inhibitory
effects
(K
i
s)
ranged
from
1.31
13.07
μM,
comparison
reference
medication
acetazolamide
(AAZ,
K
0.12
μM).
addition,
effectively
suppressed
by
these
drugs,
with
s
ranging
1.42
11.93
compared
AAZ
0.098
Significant
between
medicines
hCAs
indicated
their
support
therapeutic
targets
against
diseases.
Furthermore,
findings
acquired
will
contribute
enhancement
dose
regimens
medications
prevention
unforeseen
drug‐drug
when
administered
concurrently
other
substances.
RSC Medicinal Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
A
series
of
sulfonamides
incorporating
a
1,2,3-triazolyloxime
substituted
1,2,3-triazolyl
moiety
were
conceptualized
and
synthesized
as
human
carbonic
anhydrase
(
Pharmacology Research & Perspectives,
Год журнала:
2025,
Номер
13(2)
Опубликована: Март 24, 2025
The
research
and
design
of
new
inhibitors
for
the
treatment
diseases
such
as
Alzheimer's
disease
glaucoma
through
inhibition
cholinesterases
(ChEs;
acetylcholinesterase,
AChE
butyrylcholinesterase,
BChE)
carbonic
anhydrase
enzymes
are
among
important
targets.
Here,
a
series
novel
sulfonamide-bearing
pyrazolone
derivatives
(1a-f
2a-f)
were
successfully
synthesized
characterized
by
using
spectroscopic
analytical
methods.
inhibitory
activities
these
newly
compounds
evaluated
both
in
vitro
silico
their
effect
on
anhydrases
(hCA
I
hCA
II
isoenzymes)
ChEs.
studies
showed
that
demonstrated
potential
activity,
with
KI
values
covering
following
ranges:
18.03
±
2.86-75.54
4.91
nM
I,
24.84
1.57-85.42
6.60
II,
7.45
0.98-16.04
1.60
AChE,
34.78
5.88-135.70
17.39
BChE.
Additionally,
many
promising
some
higher
potency
than
reference
compounds.
While
have
also
identified
binding
positions
compounds,
crystal
structures
BChE
receptors.
varying
affinities
designed
ChEs
isoenzymes
show
could
hold
promise
alternative
agents
selectively
inhibiting
hCAs
glaucoma.
