Abstract
Indole‐pyrazole
hybrids
are
intriguing
due
to
their
potential
for
synergistic
pharmacological
effects,
unlike
molecules
with
only
one
pharmacophore.
This
study
presents
a
one‐pot
synthesis
of
fused
indole‐pyrazole
derivatives,
bis
4a
and
chromone
4b
using
an
aldehyde,
thiosemicarbizide,
indole,
as
anticancer
antidiabetic
agents.
The
synthesized
compounds
were
characterized
Fourier
transform
infrared
(FTIR),
nuclear
magnetic
resonance
(NMR),
time‐of‐flight
mass
spectrometry
(TOF‐MS).
Initially,
mutagenicity
test
was
performed,
the
showed
no
significant
increase
in
revertant
colonies
against
Salmonella
typhimurium
TA
98
100
strains.
In
MTT
assay
cytotoxicity
two
human
cancer
cell
lines,
A549
HepG‐2;
normal
line,
HEK
293.
Compound
high
potency
IC
50
values
18.70
50.07
µg/mL,
respectively,
whereas
both
low
inhibition
level
293
at
µg/mL.
vitro
α‐amylase
α‐glucosidase,
compound
demonstrated
excellent
3.9
µg/mL
12.1
respectively.
Molecules,
Год журнала:
2024,
Номер
29(10), С. 2277 - 2277
Опубликована: Май 12, 2024
Cancer
is
ranked
among
lethal
diseases
globally,
and
the
increasing
number
of
cancer
cases
deaths
results
from
limited
access
to
effective
therapeutics.
The
use
plant-based
medicine
has
been
gaining
interest
several
researchers.
Carvacrol
its
isomeric
compound,
thymol,
are
extracts
that
possess
biological
activities,
such
as
antimalarial,
anticancer,
antifungal,
antibacterial.
However,
their
efficacy
compromised
by
poor
bioavailability.
Thus,
medicinal
scientists
have
explored
synthesis
hybrid
compounds
containing
pharmacophores
enhance
therapeutic
improve
Hence,
this
review
a
comprehensive
report
on
carvacrol
isomer,
with
potent
anticancer
antibacterial
agents
reported
between
2020
2024.
Furthermore,
structural
activity
relationship
(SAR)
recommended
future
strategies
further
effects
will
be
discussed.
Heliyon,
Год журнала:
2024,
Номер
10(7), С. e27880 - e27880
Опубликована: Март 21, 2024
Alzheimer's
disease
(AD),
is
characterized
by
a
progressive
loss
of
cognitive
abilities
as
well
behavioral
symptoms
including
disorientation,
trouble
solving
problems,
personality
and
mood
changes.
Acetylcholinesterase
(AChE)
promising
target
for
symptomatic
improvement
in
AD
due
to
its
consistent
early
cholinergic
deficit.
This
research
has
investigated
the
potential
compounds
from
Catunaregam
spinosa
AChE
inhibitors
treatment
option
AD,
aiming
enhance
neurotransmission
alleviate
decline.
Tacrine,
FDA's
first
approved
no
longer
use
hepatotoxicity.
Box-Behnken
design
(BBD)
modelling
was
used
optimise
ultrasonic
extraction
alkaloids
dried
fruits
C.
spinosa.
GC-MS
analysis
revealed
presence
ninety
phytoconstituents
extract.
Among
them,
eighty-nine
new
are
reported
this
plant
fruit
time.
Out
phytoconstituents,
eight
showed
best
binding
affinity
against
enzyme,
i.e.,
PDB
IDs
1GQR,
1QTI
4PQE
targets
using
iGEMDOCK.
The
lead
hits
were
tested
their
drug-like
properties
atomistic
mechanisms
silico
ADMET
prediction,
LigPlot
analysis,
molecular
dynamics
simulation.
results
suggest
four
such
1,4,7,10,13,16-hexaoxacyclooctadecane;
butanoic
acid,
3-methyl-2-[(phenylmethoxy)imino]-,
trime;
butane-1,2,3,4-tetraol;
D-(+)-ribonic
acid.gamma-lactone
potent
possible
AD.
Biomedicines,
Год журнала:
2024,
Номер
12(6), С. 1192 - 1192
Опубликована: Май 27, 2024
Breast
cancer
is
the
most
common
among
women.
Currently,
it
poses
a
significant
threat
to
healthcare
system
due
emerging
resistance
and
toxicity
of
available
drug
candidates
in
clinical
practice,
thus
generating
an
urgent
need
for
development
new
potent
safer
anti-breast
candidates.
Coumarin
(chromone-2-one)
elite
ring
widely
distributed
natural
products
possesses
broad
range
pharmacological
properties.
The
unique
distribution
efficacy
coumarins
attract
product
hunters,
resulting
identification
numerous
from
different
sources
last
three
decades,
especially
those
with
Inspired
by
this,
synthetic
derivatives
based
on
have
been
developed
medicinal
chemists
all
around
globe,
showing
promising
efficacy.
This
review
primarily
focused
coumarin-inspired
agents
highlighting
design
strategies,
mechanistic
insights,
their
structure–activity
relationship.
Natural
having
are
also
briefly
highlighted.
will
act
as
guideline
researchers
designing
optimum
coumarin-based
agents.
