Archiv der Pharmazie,
Journal Year:
2021,
Volume and Issue:
355(1)
Published: Oct. 5, 2021
Abstract
Human
carbonic
anhydrase
(hCA)
isoenzymes
are
zinc
ion‐containing,
widespread
metalloenzymes
and
they
classically
play
a
role
in
pH
homeostasis
maintenance.
CA
inhibitors
suppress
the
activity
their
usage
has
been
clinically
established
as
antiglaucoma
agents,
antiepileptics,
diuretics,
some
other
disorders.
Alzheimer's
disease
(AD)
is
slowly
progressive
neurodegenerative
disorder
fatal
of
brain.
An
advanced
method
to
cure
AD
includes
strategy
design
acetylcholinesterase
(AChE)
inhibitors.
A
novel
series
pyrrole‐3‐one
derivatives
containing
sulfa
drugs
(
5a–i
)
were
determined
be
highly
potent
for
AChE
hCA
I
II
(inhibitory
constant
[
K
i
]
values
range
6.50
±
1.02–37.46
4.12
nM,
1.20
0.19–44.21
1.09
8.93
1.58–46.86
8.41
nM
AChE,
I,
II,
respectively).
The
designed
compounds
often
show
more
effective
inhibition
than
chemicals
used
standard.
Among
these
compounds,
5f
was
most
compound
against
5e
II.
It
that
5c
inhibitor
AChE.
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2020,
Volume and Issue:
39(5), P. 1672 - 1680
Published: Feb. 28, 2020
Carbonic
anhydrases
(CAs)
are
potent
dehydration
of
carbonic
acid
and
catalyst
the
reversible
hydration
carbon
dioxide.
Here,
CA
I
II
was
purified
from
human
erythrocytes
using
simple
chromatographic
method
determined
interactions
between
some
calcium
channel
blockers
enzymes.
Molecular
docking
studies
were
performed
these
compounds.
It
found
that
(nimodipine,
nilvadipine,
nitrendipine,
isradipine,
nifedipine)
exhibit
potential
inhibitor
properties
for
hCA
II.
IC50
values
in
range
9.24-58.00
μM,
Ki
constants
7.60
±
2.68-35.92
16.01
μM.
70.00-138.60
48.30
9.81-162.35
20.47
Nimodipine
presented
highest
score
had
competitive
inhibition,
benzene
pyridine
rings
to
enter
cavity
I.
Nifedipine
isradipine
did
not
affect
Among
drugs,
nitrendipine
be
most
nimodipine
These
compounds
may
useful
inhibitors.Communicated
by
Ramaswamy
H.
Sarma
European Journal of Medicinal Chemistry Reports,
Journal Year:
2022,
Volume and Issue:
5, P. 100042 - 100042
Published: April 18, 2022
Cancer
is
one
of
the
leading
causes
death
globally,
around
10
million
deaths
are
reported
every
year
due
to
cancer.
Some
clinically
approved
anticancer
drugs
play
a
riveting
role
in
its
treatment.
Still,
severe
emergence
drug
resistance,
side
effects,
and
multidrug-resistant
cancers
mutations,
it
creates
significant
demand
for
novel,
potent,
safe
candidates
as
an
agent
with
diverse
mechanisms
action.
In
medicinal
chemistry,
several
heterocyclic
derivatives
hybrids
studied
potent
agents;
Pyrazoline
versatile
ubiquitous
scaffolds
developing
novel
agents.
Many
pyrazoline
bearing
used
treatment
Few
late
phase
clinical
trial
treating
various
cancers,
example,
Indibulin,
microtubule
inhibitor
AT9283.
The
hybridization
strategy
scaffold
rings
very
promising
minimize
effects
resistance.
light
this
containing
monopolize
important
place
presented
review
outlined
recent
advances
towards
pyrazoline-containing
covers
synthetic
strategy,
structure-activity
relationship
activities
hybrid
derivatives.
sole
purpose
shed
on
design
development
compounds
high
efficacy
reduced
toxicity.
Archiv der Pharmazie,
Journal Year:
2020,
Volume and Issue:
353(10)
Published: July 9, 2020
Abstract
Coumarins
and
their
derivatives
are
receiving
increasing
attention
due
to
numerous
biochemical
pharmacological
applications.
In
this
study,
a
series
of
novel
coumarin–1,2,3‐triazole‐acetamide
hybrids
was
tested
against
some
metabolic
enzymes
including
α‐glycosidase
(α‐Gly),
α‐amylase
(α‐Amy),
acetylcholinesterase
(AChE),
butyrylcholinesterase
(BChE),
human
carbonic
anhydrase
I
(hCA
I),
hCA
II.
The
new
showed
K
i
values
in
the
range
483.50–1,243.04
nM
I,
508.55–1,284.36
II,
24.85–132.85
AChE,
27.17–1,104.36
BChE,
590.42–1,104.36
α‐Gly,
55.38–128.63
α‐Amy.
had
effective
inhibition
profiles
all
enzymes.
Also,
enzyme
inhibitory
effects
hybrids,
they
potential
drug
candidates
treat
diseases
such
as
epilepsy,
glaucoma,
type‐2
diabetes
mellitus
(T2DM),
Alzheimer's
disease
(AD),
leukemia.
Additionally,
these
were
compared
with
standard
inhibitors
like
acetazolamide
(for
II),
tacrine
AChE
BChE),
acarbose
α‐Gly
α‐Amy).
those
best
score
docked
into
active
site
indicated
