ChemMedChem,
Journal Year:
2022,
Volume and Issue:
17(5)
Published: Jan. 3, 2022
Due
to
the
ever-increasing
antimicrobial
resistance
there
is
an
urgent
need
continuously
design
and
develop
novel
agents.
Inspired
by
broad
antibacterial
activities
of
various
heterocyclic
compounds
such
as
2-quinolone
derivatives,
we
designed
synthesized
new
methyl-(2-oxo-1,2-dihydroquinolin-4-yl)-L-alaninate-1,2,3-triazole
derivatives
via
1,3-dipolar
cycloaddition
reaction
1-propargyl-2-quinolone-L-alaninate
with
appropriate
azide
groups.
The
were
obtained
in
good
yield
ranging
from
75
80
%.
chemical
structures
these
hybrid
molecules
determined
spectroscopic
methods
activity
was
investigated
against
both
bacterial
fungal
strains.
tested
showed
significant
weak
moderate
antifungal
activity.
Despite
evident
similarity
quinolone
moiety
our
fluoroquinolones,
do
not
function
inhibiting
DNA
gyrase.
Computational
characterization
shows
that
they
have
attractive
physicochemical
pharmacokinetic
properties
could
serve
templates
for
developing
potential
agents
clinical
use.
Green Chemistry,
Journal Year:
2022,
Volume and Issue:
24(13), P. 5058 - 5063
Published: Jan. 1, 2022
The
electrochemical
annulation
of
enaminones/analogous
enamines
and
thioureas
providing
2-aminothiazoles
has
been
realized.
Modulating
the
electrolyte
enables
diastereoselective
synthesis
4,5-dialkoxyl
thiazolines
by
dearomatization.
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].
Journal of Chemistry,
Journal Year:
2022,
Volume and Issue:
2022, P. 1 - 50
Published: Jan. 6, 2022
A
pharmacophore
system
has
been
found
as
1,2,3-triazole,
a
five-membered
heterocycle
ring
with
nitrogen
heteroatoms.
These
heterocyclic
compounds
can
be
produced
using
azide-alkyne
cycloaddition
processes
catalyzed
by
ruthenium
or
copper.
The
bioactive
demonstrated
antitubercular,
antibacterial,
anti-inflammatory,
anticancer,
antioxidant,
antiviral,
and
antidiabetic
properties.
This
molecule,
in
particular,
one
more
1,2,3-triazole
cores
to
have
the
most
powerful
antifungal
effects.
goal
of
this
review
is
highlight
recent
developments
synthesis
structure-activity
relationship
(SAR)
investigation
prospective
fungicidal
chemical.
Also
there
explained
drugs
mechanism
action
triazole
compound
activity.
will
useful
variety
fields,
including
medicinal
chemistry,
organic
mycology,
pharmacology.
Pharmaceutics,
Journal Year:
2024,
Volume and Issue:
16(1), P. 89 - 89
Published: Jan. 9, 2024
Antimicrobial
resistance
is
an
increasing
problem
for
global
public
health.
One
of
the
strategies
to
combat
this
issue
synthesis
novel
antimicrobials
through
rational
drug
design
based
on
extensive
structure–activity
relationship
studies.
The
thiazole
nucleus
a
prominent
feature
in
structure
many
authorized
antimicrobials,
being
clubbed
with
different
heterocycles.
purpose
review
study
antimicrobial
thiazoles
various
heterocycles,
as
reported
literature
between
2017
and
2023,
order
offer
overview
last
years
terms
research
provide
helpful
instrument
future
field.
Current Topics in Medicinal Chemistry,
Journal Year:
2021,
Volume and Issue:
22(1), P. 41 - 63
Published: Nov. 12, 2021
Staphylococcus
aureus
(S.
aureus),
a
prominent,
highly
contagious
nosocomial
and
community-
acquired
bacterial
pathogen,
can
cause
broad
spectrum
of
diseases.
Antibiotic-resistant
S.
strains,
which
pose
potential
causes
morbidity
mortality,
have
continuously
emerged
in
recent
years,
calling
for
novel
anti-S.
agents.
1,2,3-triazole
1,2,4-triazole,
the
bioisostere
amides,
esters,
carboxylic
acids,
are
potent
inhibitors
DNA
gyrase,
topoisomerase
IV,
efflux
pumps,
filamentous
temperature-sensitive
protein
Z,
penicillin-binding
protein.
In
particular,
1,2,3-triazole-
1,2,4-triazole-containing
hybrids
to
exert
dual
or
multiple
antibacterial
mechanisms
action.
Moreover,
1,2,3-triazole-cephalosporin
hybrid
cefatrizine,
1,2,3-
triazole-oxazolidinone
radezolid,
1,2,4-triazolo[1,5-a]pyrimidine
essramycin,
already
been
used
clinical
practice
treat
infections.
Hence,
1,2,4-
triazole-containing
possess
promising
broad-spectrum
activity
against
diverse
clinically
significant
organisms,
including
drug-resistant
forms.
This
review
is
an
update
on
latest
development
with
activity,
covering
articles
published
between
January
2020
July
2021.
