Future Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
15(4), P. 345 - 363
Published: Feb. 1, 2023
Aim:
α-Glucosidase
inhibitors
are
important
oral
antidiabetic
drugs
that
used
alone
or
in
combination
therapy.
Materials
&
methods:
In
this
regard,
1,3,4-thiadiazoles–1,2,3-triazoles
were
designed,
synthesized
and
evaluated
for
α-glucosidase
enzyme
inhibition.
Results:
The
applied
synthesis
protocol
involved
a
'click'
reaction
between
novel
alkyne
derived
from
1,3,4-thiadiazole
derivative
phenylacetamide
azides.
hybrid
(9n)
bearing
2-methyl
4-nitro
substituents
was
the
best
inhibitor
with
an
IC50
value
of
31.91
μM
(acarbose
=
844.81
μM).
blind
molecular
docking
study
showed
it
interacted
allosteric
site's
amino
acid
residues
α-glucosidase.
Conclusion:
'Click'-inspired
potential
(1,3,4-thiadiazole–1,2,3-triazole
hybrids)
identified
structure–activity
relationship
kinetic
studies
accomplished.
Frontiers in Chemistry,
Journal Year:
2022,
Volume and Issue:
10
Published: Sept. 26, 2022
Triazole,
comprising
three
nitrogen
atoms
and
two
carbon
atoms,
is
divided
into
isomers
1,2,3-triazole
1,2,4-triazole.
Compounds
containing
a
triazole
are
one
of
the
significant
heterocycles
that
exhibit
broad
biological
activities,
such
as
antimicrobial,
analgesic,
anti-inflammatory,
anticonvulsant,
antineoplastic,
antimalarial,
antiviral,
antiproliferative,
anticancer
activities.
A
great
quantity
drugs
with
structure
has
been
developed
proved,
for
example,
ketoconazole
fluconazole.
Given
importance
scaffold,
its
synthesis
attracted
much
attention.
This
review
summarizes
synthetic
methods
compounds
from
various
sources
in
past
20
years.
Antibiotics,
Journal Year:
2023,
Volume and Issue:
12(7), P. 1220 - 1220
Published: July 22, 2023
Bacterial
infections
have
attracted
the
attention
of
researchers
in
recent
decades,
especially
due
to
special
problems
they
faced,
such
as
their
increasing
diversity
and
resistance
antibiotic
treatment.
The
emergence
development
SARS-CoV-2
infection
stimulated
even
more
research
find
new
structures
with
antimicrobial
antiviral
properties.
Among
heterocyclic
compounds
remarkable
therapeutic
properties,
benzimidazoles,
triazoles
stand
out,
possessing
antimicrobial,
antiviral,
antitumor,
anti-Alzheimer,
anti-inflammatory,
analgesic,
antidiabetic,
or
anti-ulcer
activities.
In
addition,
literature
last
decade
reports
benzimidazole-triazole
hybrids
improved
biological
properties
compared
simple
mono-heterocyclic
compounds.
This
review
aims
provide
an
update
on
synthesis
methods
these
hybrids,
along
activities,
well
structure-activity
relationship
reported
literature.
It
was
found
that
presence
certain
groups
grafted
onto
benzimidazole
and/or
triazole
nuclei
(-F,
-Cl,
-Br,
-CF3,
-NO2,
-CN,
-CHO,
-OH,
OCH3,
COOCH3),
some
heterocycles
(pyridine,
pyrimidine,
thiazole,
indole,
isoxazole,
thiadiazole,
coumarin)
increases
activity
hybrids.
Also,
oxygen
sulfur
atom
bridge
connecting
rings
generally
mentions
only
benzimidazole-1,2,3-triazole
Both
for
additional
ring
activity,
which
is
agreement
three-dimensional
binding
mode
summarizes
advances
derivatives
potential
agents
covering
articles
published
from
2000
2023.
ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(18)
Published: May 6, 2024
Abstract
Multicomponent
reactions
are
operationally
simple
and
display
a
significant
role
in
diverse
chemical
modification
by
reducing
reaction
times
as
well
additional
steps
involved.
In
this
review,
we
highlighted
the
impact
of
multi‐component
assistance
with
modular
Click
chemistry
to
develop
library
triazole‐appended
scaffolds
including
1,2,3‐triazole‐fused
heterocycles,
glycoconjugates,
macrocycles
combinatorial
synthesis
differently
functionalized
triazoles
along
mechanistic
insights
range
applications
field
medicinal
chemistry.
Current Organic Synthesis,
Journal Year:
2023,
Volume and Issue:
21(4), P. 513 - 558
Published: April 19, 2023
Immediately
after
the
invention
of
'Click
Chemistry'
in
2002,
regioselective
1,2,3-
triazole
scaffolds
resulted
from
respective
organic
azides
and
terminal
alkynes
under
Cu(I)
catalysis
have
been
well
recognized
as
functional
heterocyclic
core
at
centre
modern
chemistry,
medicinal
material
sciences.
This
CuAAC
reaction
has
several
notable
features
including
excellent
regioselectivity,
high-to-excellent
yields,
easy
to
execute,
short
time,
modular
nature,
mild
condition,
readily
available
starting
materials,
etc.
Moreover,
resulting
triazoles
can
serve
amide
bond
isosteres,
a
privileged
group
drug
discovery
development.
More
than
hundreds
reviews
had
devoted
special
reference
1,4-disubstituted
triazoles,
while
only
little
efforts
were
made
for
an
opposite
regioisomer
i.e.,
1,5-disubstituted
triazole.
Herein,
we
presented
various
classical
approaches
expeditious
synthesis
wide
range
biologically
relevant
1,5-
disubstituted
1,2,3-triazole
analogues.
The
syntheses
such
class
diversly
functionalized
emerged
crucial
investigation
domain
chemistry
biology.
tutorial
review
covers
literature
assessment
on
development
synthetic
protocols
reported
during
last
12
years.
Chemistry - A European Journal,
Journal Year:
2023,
Volume and Issue:
29(55)
Published: July 11, 2023
A
novel
organocatalyzed
[3+2]
cycloaddition
reaction
of
nitroolefins
with
glycosyl
azides
as
well
organic
has
been
developed
for
successful
construction
1,5-disubstituted
triazolyl
glycoconjugates.
This
metal-free
and
acid-free,
regioselective
synthetic
protocol
proceeds
in
the
presence
only
Schreiner
thiourea
organocatalysts,
which
enable
required
activation
through
double
hydrogen
bonding.
The
straightforward,
operationally
simple,
regioselectivity
this
methodology,
complementing
to
classical
RuAAC
catalyzed
synthesis
1,2,3-triazoles.
In
catalytic
amount
organocatalyst,
react
a
broad
array
producing
series
diverse
1,2,3-
triazoles
good
yields
excellent
regioselectivity.
The Chemical Record,
Journal Year:
2023,
Volume and Issue:
23(11)
Published: July 31, 2023
Abstract
Click
Chemistry,
a
modular,
rapid,
and
one
of
the
most
reliable
tool
for
regioselective
1,2,3‐triazole
forming
[3+2]
reaction
organic
azide
terimal
alkyne
is
widely
explored
in
various
emerging
domains
research
ranging
from
chemical
biology
to
catalysis
medicinal
chemistry
material
science.
This
diverse
range
azido‐alkyne
scaffolds
has
been
well
performed
both
intermolecular
as
intramolecular
fashions.
In
comparison
metal
(Cu/Ru/Ni)
variant
‘Click
Chemistry’,
click
little
addressed.
The
exemplified
mordern
cyclization
which
involves
metal‐catalyzed
(CuAAC/RuAAC)
cyclization,
organo‐catalyzed
thermal‐induced
topochemical
reaction.
Thus,
we
report
herein
recent
approaches
on
azide‐alkyne
cycloaddition
Chemistry‘
with
their
wide‐spread
applications
developement
molecules
including
fused‐heterocycles,
well‐defined
peptidomemics,
macrocyclic
architectures
notable
features.
