ChemistrySelect,
Journal Year:
2025,
Volume and Issue:
10(2)
Published: Jan. 1, 2025
Abstract
A
lot
of
interest
has
been
gained
recently
in
developing
novel
acetylcholinesterase
(AChE)
inhibitors
that
can
alleviate
Alzheimer's
symptoms.
In
the
current
study,
we
aimed
to
explore
AChE
inhibitory
activity
new
chromenes
attached
1,3,4‐oxadiazole
and/or
pyrazole
units.
The
hybrids
were
obtained
via
[3
+
2]
cycloaddition
reaction
between
appropriate
chromene‐based
enaminones
and
hydrazonyl
chlorides.
inhibition
percentages
products
against
recorded
at
tested
concentrations
15
25
µM
compared
donepezil.
3‐(3‐Acetyl‐1‐(4‐methoxyphenyl)‐1
H
‐pyrazole‐4‐carbonyl)‐6‐(((5‐phenyl‐1,3,4‐oxadiazol‐2‐yl)thio)methyl)‐2
‐chromen‐2‐one
displayed
promising
with
73.2
87.3,
respectively,
aforementioned
concentrations.
Moreover,
previous
hybrid
gave
2,2‐diphenylpicrylhydrazyl
(DPPH)
using
reference
ascorbic
acid.
It
had
an
percentage
86.6
a
concentration
µM.
European Journal of Medicinal Chemistry Reports,
Journal Year:
2024,
Volume and Issue:
12, P. 100185 - 100185
Published: July 2, 2024
Fused
thienopyridines
represent
a
class
of
heterocyclic
molecules
that
have
garnered
increasing
attention
due
to
their
unique
structural
features
and
versatile
chemical
properties.
This
review
systematically
examines
the
latest
synthetic
methodologies
employed
in
preparing
fused
thienopyridine
derivatives,
emphasizing
innovative
approaches
contribute
diversity.
Moreover,
discussion
extends
broad
spectrum
therapeutic
applications
offer,
encompassing
utility
different
diseases.
The
explores
pharmacological
activities
biological
properties
thienopyridines,
shedding
light
on
role
drug
discovery
development.
By
offering
comprehensive
overview
recent
advancements
both
synthesis
this
will
serve
as
valuable
resource
for
researchers
practitioners
navigating
evolving
landscape
medicinal
chemistry.
Current Alzheimer Research,
Journal Year:
2023,
Volume and Issue:
20(3), P. 131 - 148
Published: March 1, 2023
The
accumulation
of
amyloid-β
(Aβ)
is
the
main
event
related
to
Alzheimer's
disease
(AD)
progression.
Over
years,
several
disease-modulating
approaches
have
been
reported,
but
without
clinical
success.
amyloid
cascade
hypothesis
evolved
and
proposed
essential
targets
such
as
tau
protein
aggregation
modulation
β-secretase
(β-site
precursor
cleaving
enzyme
1
-
BACE-1)
γ-secretase
proteases.
BACE-1
cuts
(APP)
release
C99
fragment,
giving
rise
Aβ
peptide
species
during
subsequent
cleavage.
In
this
way,
has
emerged
a
clinically
validated
attractive
target
in
medicinal
chemistry,
it
plays
crucial
role
rate
generation.
review,
we
report
results
candidates
trials
E2609,
MK8931,
AZD-3293,
addition
highlighting
pharmacokinetic
pharmacodynamic-related
effects
inhibitors
already
reported.
current
status
developing
new
peptidomimetic,
non-peptidomimetic,
naturally
occurring,
other
class
are
demonstrated,
considering
their
limitations
lessons
learned.
goal
provide
broad
complete
approach
subject,
exploring
chemical
classes
perspectives.
