European Journal of Medicinal Chemistry Reports,
Journal Year:
2023,
Volume and Issue:
9, P. 100113 - 100113
Published: Sept. 7, 2023
Natural
products
play
a
key
role
in
the
history
of
human
drug
discovery,
and
especially
for
anticancer
agents.
Copper(I)-catalyzed
alkyne-azide
[3+2]
cycloaddition
(CuAAC)
reaction
is
perhaps
most
powerful
method
efficient
modification
complex
natural
products,
enabling
direct
incorporation
various
functional
groups
accompanied
by
formation
multifunctional
1,2,3-triazole
motif,
which
could
not
only
serve
as
an
basic
hydrophilic
connecting
group
but
also
bioisosteres
5-
or
6-membered
heterocycles
amide
group,
thus
facilitating
improvement
activities
and/or
drug-like
properties.
This
contribution
extensively
summarizes
state-of-the-art
application
activity.
The
aim
to
gain
deep
understanding
fruitful
achievements
well
limitations
CuAAC
click
chemistry
product
activity,
provide
perspectives
directions
regarding
future
studies
medicinal
chemistry.
Pharmaceuticals,
Journal Year:
2023,
Volume and Issue:
16(2), P. 179 - 179
Published: Jan. 24, 2023
Acetylcholine
(ACh)
neurotransmitter
of
the
cholinergic
system
in
brain
is
involved
learning,
memory,
stress
responses,
and
cognitive
functioning.
It
hydrolyzed
into
choline
acetic
acid
by
two
key
cholinesterase
enzymes,
viz.,
acetylcholinesterase
(AChE)
butyrylcholinesterase
(BuChE).
A
loss
or
degeneration
neurons
that
leads
to
a
reduction
ACh
levels
considered
significant
contributing
factor
development
neurodegenerative
diseases
(NDs)
such
as
Alzheimer’s
disease
(AD).
Numerous
studies
have
shown
inhibitors
can
raise
level
and,
therefore,
enhance
people’s
quality
life,
at
very
least,
it
temporarily
lessen
symptoms
NDs.
1,2,3-triazole,
five-membered
heterocyclic
ring,
privileged
moiety,
is,
central
scaffold,
capable
interacting
with
variety
receptors
enzymes
exhibit
broad
range
important
biological
activities.
Recently,
has
been
clubbed
other
pharmacophoric
fragments/molecules
hope
obtaining
potent
selective
AChE
and/or
BuChE
inhibitors.
The
present
updated
review
succinctly
summarizes
different
synthetic
strategies
used
synthesize
1,2,3-triazole
moiety.
also
highlights
anticholinesterase
potential
various
di/trihybrids
reported
past
seven
years
(2015–2022),
including
rationale
for
hybridization
an
emphasis
on
their
structural
features
optimization
treat
Scientific Reports,
Journal Year:
2024,
Volume and Issue:
14(1)
Published: March 23, 2024
Abstract
A
series
of
novel
1,2,3-triazole
and
chiral
Schiff
base
hybrids
2
–
6
were
synthesized
by
condensation
reaction
from
pre-prepared
parent
component
the
(1,2,3-triazole
1)
primary
amines
their
chemical
structure
confirmed
using
NMR
FTIR
spectroscopies,
CHN
elemental
analysis.
Compounds
1
evaluated
for
anticancer
activity
against
two
cancer
PC3
(prostate)
A375
(skin)
MRC-5
(healthy)
cell
lines
Almar
Blue
assay
method.
The
compounds
exhibited
significant
cytotoxicity
tested
lines.
Among
3
showed
very
good
inhibition
low
toxicity
healthy
All
high
binding
affinity
Androgen
receptor
modulators
(PDB
ID:
5t8e)
Human
MIA
1i1j)
inhibitors
compared
to
reference
drug
(cisplatin).
Structure
relationships
(SARs)
is
in
agreement
with
DFT
molecular
docking
studies.
desirable
physicochemical
properties
likeness.
Frontiers in Pharmacology,
Journal Year:
2021,
Volume and Issue:
12
Published: June 11, 2021
Lung
cancer
is
the
most
common
malignancy
and
leads
to
around
one-quarter
of
all
deaths.
Great
advances
have
been
achieved
in
treatment
lung
with
novel
anticancer
agents
improved
technology.
However,
morbidity
mortality
rates
remain
extremely
high,
calling
for
an
urgent
need
develop
anti-lung
agents.
1,2,3-Triazole
could
be
readily
interact
diverse
enzymes
receptors
organisms
through
weak
interaction.
can
not
only
acted
as
a
linker
tether
different
pharmacophores
but
also
serve
pharmacophore.
This
review
aims
summarize
recent
1,2,3-triazole-containing
compounds
potential,
their
structure-activity
relationship
(SAR)
together
mechanisms
action
discussed
pave
way
further
rational
development
candidates.
Expert Opinion on Drug Discovery,
Journal Year:
2022,
Volume and Issue:
17(11), P. 1209 - 1236
Published: Sept. 27, 2022
The
1,2,3-triazole
ring
occupies
an
important
space
in
medicinal
chemistry
due
to
its
unique
structural
properties,
synthetic
versatility
and
pharmacological
potential
making
it
a
critical
scaffold.
Since
is
readily
available
through
click
for
creating
compound
collections
against
various
diseases,
has
become
emerging
area
of
interest
chemists.This
review
article
addresses
the
properties
the1,2,3-triazole
nucleus
as
intriguing
system
drug
discovery
while
focusing
on
most
recent
strategies
exploited
design
development
analogs
inhibitors
biological
targets.Evidently,
with
features
enormous
diseases
pharmacophore,
bioisoster
or
platform.
evidence
indicates
that
may
be
more
molecules
near
future
along
increasing
understanding
prominent
roles
structures.
feasibility
triazole
make
certainly
ideal
libraries
constructive
structure-activity
relationship
studies.
However,
comparative
target-specific
studies
are
needed
gain
deeper
molecular
recognition.[Figure:
see
text].
