RSC Advances,
Год журнала:
2022,
Номер
12(30), С. 19640 - 19666
Опубликована: Янв. 1, 2022
This
review
article
demonstrates
the
various
synthetic
pathways
of
five-membered
nitrogen-containing
heterocycles
such
as
pyrroles,
pyrazoles,
imidazoles,
triazoles
and
tetrazoles
catalysed
by
metallic
nanocatalysts.
Molecules,
Год журнала:
2021,
Номер
26(14), С. 4213 - 4213
Опубликована: Июль 11, 2021
Nitrogen-containing
heterocyclic
rings
are
common
structural
components
of
marketed
drugs.
Among
these
heterocycles,
imidazole/fused
imidazole
present
in
a
wide
range
bioactive
compounds.
The
unique
properties
such
structures,
including
high
polarity
and
the
ability
to
participate
hydrogen
bonding
coordination
chemistry,
allow
them
interact
with
biomolecules,
imidazole-/fused
imidazole-containing
compounds
reported
have
broad
spectrum
biological
activities.
This
review
summarizes
recent
reports
derivatives
as
anticancer
agents
appearing
peer-reviewed
literature
from
2018
through
2020.
Such
molecules
been
shown
modulate
various
targets,
microtubules,
tyrosine
serine-threonine
kinases,
histone
deacetylases,
p53-Murine
Double
Minute
2
(MDM2)
protein,
poly
(ADP-ribose)
polymerase
(PARP),
G-quadraplexes,
other
targets.
Imidazole-containing
that
display
activity
by
unknown/undefined
mechanisms
also
described,
well
key
features
structure-activity
relationships.
is
intended
provide
an
overview
advances
imidazole-based
drug
discovery
development,
inspire
design
synthesis
new
molecules.
Journal of Genetic Engineering and Biotechnology,
Год журнала:
2020,
Номер
18(1), С. 69 - 69
Опубликована: Ноя. 3, 2020
The
COVID-19
pandemic
caused
by
SARS-CoV-2
has
shown
an
exponential
trend
of
infected
people
across
the
planet.
Crediting
its
virulent
nature,
it
becomes
imperative
to
identify
potential
therapeutic
agents
against
deadly
virus.
3-chymotrypsin-like
protease
(3CLpro)
is
a
cysteine
which
causes
proteolysis
replicase
polyproteins
generate
functional
proteins,
crucial
step
for
viral
replication
and
infection.
Computational
methods
have
been
applied
in
recent
studies
promising
inhibitors
3CLpro
inhibit
activity.
This
review
provides
overview
drug/lead
candidates
identified
so
far
through
various
silico
approaches
such
as
structure-based
virtual
screening
(SBVS),
ligand-based
(LBVS)
drug-repurposing/drug-reprofiling/drug-retasking.
Further,
drugs
classified
according
their
chemical
structures
or
biological
activity
into
flavonoids,
peptides,
terpenes,
quinolines,
nucleoside
nucleotide
analogues,
inhibitors,
phenalene
antibiotic
derivatives.
These
are
then
individually
discussed
based
on
structural
parameters
namely
estimated
free
energy
binding
(ΔG),
key
interacting
residues,
types
intermolecular
interactions
stability
3CLpro-ligand
complexes
obtained
from
results
molecular
dynamics
(MD)
simulations.
comprehensive
information
several
computational
thus
better
understanding
interaction
patterns
dynamic
states
ligand-bound
structures.
Chinese Journal of Chemistry,
Год журнала:
2021,
Номер
39(8), С. 2251 - 2263
Опубликована: Май 1, 2021
Main
observation
and
conclusion
The
limit
ability
of
traditional
antibiotics
to
treat
drug
resistant
bacteria
calls
for
new
therapeutic
alternatives.
A
class
unique
sulfanilamide
aminophosphonates
as
potential
agents
against
microbes
was
synthesized
by
one‐pot
three‐component
reaction.
Noticeably,
fluorobenzyl
derivative
5d
(MIC
=
2
μg/mL)
active
E.
coli
infection
exerted
no
obvious
toxicity
towards
human
mammalian
cells.
Compound
also
displayed
good
anti‐biofilm
activity
low
possibility
induce
resistance.
Mechanism
investigation
elucidated
that
molecule
could
disrupt
membrane
through
generation
reactive
oxygen
(ROS)
then
intercalate
into
deoxyribonucleic
acid
(DNA)
form
a
steady
5d‐DNA
complex,
which
led
bacterial
death.
These
results
indicated
would
shed
light
on
developing
novel
antibacterial
agents.
Molecules,
Год журнала:
2023,
Номер
28(6), С. 2751 - 2751
Опубликована: Март 18, 2023
Several
nitrogen
heterocyclic
analogues
have
been
applied
to
clinical
practice,
and
about
75%
of
drugs
approved
by
the
FDA
contain
at
least
a
moiety.
Thus,
heterocycles
are
beneficial
scaffolds
that
occupy
central
position
in
development
new
drugs.
The
fact
certain
compounds
significantly
activate
NRF2/ARE
signaling
pathway
upregulate
expression
NRF2-dependent
genes,
especially
HO-1
NQO1,
underscores
need
study
roles
pharmacological
effects
N-based
moieties
NRF2
activation.
Furthermore,
exhibit
significant
antioxidant
anti-inflammatory
activities.
NRF2-activating
molecules
tremendous
research
interest
recent
times
due
their
therapeutic
neuroinflammation
oxidative
stress-mediated
diseases.
A
comprehensive
review
NRF2-inducing
activities
derivatives
will
broaden
prospects
wide
range
present
review,
as
first
its
kind,
provides
an
overview
activation
underpinning
actions
several
diseases,
properties
structural–activity
relationship
also
discussed
with
aim
making
discoveries
stimulate
innovative
this
area.
Abstract
Nitrogen‐containing
heterocycles
such
as
imidazoles,
thiazoles,
and
oxazoles
play
a
significant
role
in
the
fields
of
biological
pharmaceutical
chemistry.
These
compounds
were
widely
used
for
agrochemical,
pesticide,
medicinal,
industrial
applications.
Due
to
wide
spectrum
structural
diversity
well
activity
N
‐heterocycles,
plethora
reports
on
their
synthesis
have
appeared
last
few
decades.
However,
developments
various
bond‐forming
strategies
C−C,
C−N,
C−O,
C−S,
N−N,
C−H
activation,
been
powerful
synthetic
tool
derive
copious
‐heterocycles.
The
most
prominent
fascinating
imidazole,
thiazole,
oxazoles,
benzimidazole
moieties
by
C−C
C−N
coupling
reactions,
multi‐component
cycloaddition
etc.
are
discussed
this
study.
studies
demonstrated
enormous
potential
methods
accelerating
modern
chemical
establishing
molecular
beauty
through
bonding.
aspects
methodologies,
like
optimized
conditions,
substrate
scope,
mechanistic
investigations,
detail.
ACS Catalysis,
Год журнала:
2020,
Номер
11(1), С. 82 - 87
Опубликована: Дек. 14, 2020
Thiobenzoic
acid
(TBA)
can
serve
as
a
single-electron
reducing
agent
under
photoirradiation
from
blue
light-emitting
diode,
in
the
presence
of
appropriate
electron
acceptors,
and
resulting
sulfur-centered
radical
species
undergoes
hydrogen
atom
abstraction.
This
dual-role
catalysis
by
TBA
enables
regioselectivie
Cα–H
arylation
benzylamines,
benzyl
alcohols,
ethers,
well
dihydroimidazoles,
with
cyano(hetero)arenes
good
yield,
without
need
for
transition-metal
photocatalyst
and/or
synthetically
elaborated
organic
dyes.