Biomedicines,
Journal Year:
2023,
Volume and Issue:
11(1), P. 219 - 219
Published: Jan. 14, 2023
A
series
of
fourteen
pyrimido[1,2-a]benzimidazole
compounds
was
prepared
by
straightforward
heterocyclic
chemistry
and
oxidation
methods.
The
new
pyrimidobenzimidazole
derivative
2a
with
a
3-fluorophenyl
substituent
identified
as
antiparasitic
compound
showing
excellent
activities
against
Leishmania
major
parasites.
highly
active
L.
promastigotes
amastigotes
EC50
values
in
the
nanomolar
concentration
range.
Compound
3b
less
than
major,
but
more
Toxoplasma
gondii
considerable
selectivity.
Hence,
two
promising
selective
drug
candidates
for
treatment
parasitic
diseases
were
identified,
which
can
be
green
methods
using
simple
one-pot
reactions
procedures,
respectively.
Molecules,
Journal Year:
2024,
Volume and Issue:
29(10), P. 2232 - 2232
Published: May 10, 2024
Viruses
are
a
real
threat
to
every
organism
at
any
stage
of
life
leading
extensive
infections
and
casualties.
N-heterocycles
can
affect
the
viral
cycle
many
points,
including
entrance
into
host
cells,
genome
replication,
production
novel
species.
Certain
also
stimulate
host’s
immune
system,
producing
antiviral
cytokines
chemokines
that
stop
reproduction
viruses.
This
review
focused
on
recent
five-
or
six-membered
synthetic
N-heterocyclic
molecules
showing
activity
through
SAR
analyses.
The
will
assist
in
identifying
robust
scaffolds
might
be
utilized
create
effective
drugs
with
either
no
few
side
effects.
ACS Chemical Neuroscience,
Journal Year:
2024,
Volume and Issue:
15(9), P. 1828 - 1881
Published: April 22, 2024
Neurodegenerative
diseases
(NDs)
are
one
of
the
prominent
health
challenges
facing
contemporary
society,
and
many
efforts
have
been
made
to
overcome
(or)
control
it.
In
this
research
paper,
we
described
a
practical
one-pot
two-step
three-component
reaction
between
3,4-dihydronaphthalen-1(2H)-one
(1),
aryl(or
heteroaryl)glyoxal
monohydrates
(2a–h),
hydrazine
monohydrate
(NH2NH2•H2O)
for
regioselective
preparation
some
3-aryl(or
heteroaryl)-5,6-dihydrobenzo[h]cinnoline
derivatives
(3a–h).
After
synthesis
characterization
mentioned
cinnolines
(3a–h),
in
silico
multi-targeting
inhibitory
properties
these
heterocyclic
scaffolds
investigated
upon
various
Homo
sapiens-type
enzymes,
including
hMAO-A,
hMAO-B,
hAChE,
hBChE,
hBACE-1,
hBACE-2,
hNQO-1,
hNQO-2,
hnNOS,
hiNOS,
hPARP-1,
hPARP-2,
hLRRK-2(G2019S),
hGSK-3β,
hp38α
MAPK,
hJNK-3,
hOGA,
hNMDA
receptor,
hnSMase-2,
hIDO-1,
hCOMT,
hLIMK-1,
hLIMK-2,
hRIPK-1,
hUCH-L1,
hPARK-7,
hDHODH,
which
confirmed
their
functions
roles
neurodegenerative
(NDs),
based
on
molecular
docking
studies,
obtained
results
were
compared
with
wide
range
approved
drugs
well-known
(with
IC50,
EC50,
etc.)
compounds.
addition,
ADMET
prediction
analysis
was
performed
examine
prospective
drug
synthesized
compounds
The
from
studies
ADMET-related
data
demonstrated
that
series
heteroaryl)-5,6-dihydrobenzo[h]cinnolines
especially
hit
ones,
can
really
be
turned
into
potent
core
new
treatment
and/or
due
having
reactionable
locations,
they
able
further
organic
reactions
(such
as
cross-coupling
reactions),
expansion
(for
example,
using
other
types
monohydrates)
makes
avenue
designing
novel
efficient
purpose.
Applied Organometallic Chemistry,
Journal Year:
2025,
Volume and Issue:
39(3)
Published: Feb. 5, 2025
ABSTRACT
A
novel
Schiff
base
ligand
derived
from
1,2,4‐triazole‐3‐thione
was
synthesized
and
complexed
with
platinum
(IV)
ion
to
enhance
its
bioactivity.
Characterization
techniques,
including
FTIR,
NMR,
UV‐Vis,
mass
spectrometry,
confirmed
the
formation
of
molecule
revealed
that
Pt(IV)
complex
has
an
octahedral
geometry.
The
antibacterial
antifungal
activity
compounds
evaluated
against
Staphylococcus
epidermidis
,
Pseudomonas
aeruginosa
Candida
albicans
Aspergillus
flavus
metal
outperforming
ligand.
antioxidant
properties
were
using
a
DPPH
assay,
demonstrating
superior
radical‐scavenging
ability.
Cytotoxicity
studies
via
MTT
assays
on
MCF‐7
breast
cancer
cells
showed
dose‐dependent
reductions
in
cell
viability,
inducing
enhanced
antiproliferative
effects
compared
DFT
calculations
performed
investigate
electronic
compounds,
molecular
docking
conducted
alpha
estrogen
receptor
(PDB
ID:
3ERT)
predict
their
binding
affinities.
results
demonstrated
exhibited
higher
biological
than
free
ligand,
suggesting
potential
as
effective
therapeutic
agent.
ChemistrySelect,
Journal Year:
2025,
Volume and Issue:
10(7)
Published: Feb. 1, 2025
Abstract
In
recent
years,
heterocyclic
compounds
have
gained
significant
interest
due
to
their
tremendous
application
in
the
medicinal,
optical,
and
biological
fields.
Among
them,
thiazole
is
an
important
heterocycle
containing
nitrogen‐
sulfur‐
ring,
which
stands
out
as
best
for
its
pharmacological
activity.
One
of
routes
synthesize
these
molecules
through
multicomponent
reactions.
Being
a
sustainable
methodology,
it
gives
insights
into
generating
extensive
range
biologically
active
molecules.
This
review
focuses
on
significance
three‐component
four‐component
syntheses
under
various
conditions
from
year
2000
late
2024,
are
particularly
ability
produce
derivatives
with
good
yields.
