Al-Mağallaẗ al-ʻirāqiyyaẗ li-l-ṣaydalaẗ,
Год журнала:
2024,
Номер
0(0), С. 1 - 7
Опубликована: Ноя. 25, 2024
Background:
1,4-dioxane
(DX)
was
first
discovered
in
1863
and
has
been
made
accessible
for
commercial
purposes
around
the
1930s
as
a
solvent
cellulose
production
of
plastics.
Aim:
The
purpose
this
review
to
highlight
chemistry
DX
well
its
various
reported
pharmacological
toxicological
attributes.
Methods:
reviewed
data
abstracted
by
using
some
scientific
platforms,
such
Google
Scholar,
Scopus,
Web
Science,
with
no
limitation
publishing
date.
Results:
Chemically,
is
an
organic
heterocyclic
molecule
that
can
be
described
ether
found
colorless
liquid
slightly
sweet
smell,
akin
diethyl
ether.
Also,
old
usually
referred
dioxane
because
other
structural
isomers
(1,2-
1,3-)
are
seldom
encountered.
Given
pharmacokinetic
profile,
quickly
entirely
absorbed
after
oral
intake
inhalation
exposure,
cutaneous
route
accounting
substantially
less
absorption.
main
product
metabolism
humans
rats
β-hydroxy
ethoxy
acetic
acid,
which
urine-eliminated
metabolite.
Pharmacologically,
it
derivatives
have
therapeutic
benefits
against
cancer
general
hematologic
malignancies
particular.
studied
function
antimicrobial
prospect
pathogenic
microbes.
Depending
on
dose
time
frame,
cause
two
types
toxicity,
including
acute
chronic,
attributes
each.
Conclusion:
Based
examined
information,
possible
employ
bioactive
scaffold
developing
potent
antitumor
agents
serve
better
therapeutics.
Abstract
In
this
work,
we
reported
the
synthesis
of
a
novel
series
isatin‐incorporated
thiazolyl‐coumarin
derivatives
4(a–h)
by
one‐pot
three‐component
reaction
substituted
isatin,
thiosemicarbazide,
and
3‐(2‐bromoacetyl)
coumarin.
The
structures
coumarin‐thiazole
scaffolds
were
precisely
established
their
IR,
NMR,
HRMS
spectral
data.
UV–Vis
absorption
study
target
molecules
was
investigated
in
six
different
solvents.
Geometrical
optimization,
molecular
electrostatic
potential
regions,
quantum
chemical
parameters
assessed
using
density
functional
theory
(DFT)
to
explore
electronic
properties
derivatives.
synthesized
compounds
screened
for
vitro
antimycobacterial
activity
against
Mycobacterium
tuberculosis
;
all
exhibited
excellent
antitubercular
efficacy
with
MIC
≤
3.25
µg/mL;
among
them,
4c
4f
most
potent
1.56
µg/mL.
Furthermore,
silico
docking
analyses
enoyl‐ACP
reductase
(InhA)
enzyme
conducted;
ligands
demonstrated
favorable
binding
interactions
within
active
site
InhA
enzyme.
Results in Chemistry,
Год журнала:
2024,
Номер
8, С. 101611 - 101611
Опубликована: Июнь 1, 2024
Despite
the
up-to-date
advancements
in
its
treatment,
cancer
is
still
being
harvested
lives
of
millions
people
annually;
this
health
threat
necessitates
exploring
more
potent
agents
that
can
effectively
fight
it.
The
class
heterocycles
known
as
coumarin,
and
natural
synthetic
derivatives
are
thought
to
be
biomedically
valuable.
Coumarins
have
low
side
effects,
outstanding
selectivity,
a
straightforward
design
for
maximum
efficiency,
various
pharmacological
actions.
For
these
characteristics,
coumarins
continuously
isolated
from
sources
synthesized
laboratories,
alongside
with
examining
them
possible
bioactivities.
In
addition
garnering
significant
attention,
coumarin
has
emerged
valuable
scaffold
potentially
important
precursor
development
innovative
anticancer
medicines.
Researchers
working
create
new
cancer-fighting
coumarins,
well
investigating
old
ones.
Integration
two
or
cyclic
moieties
into
single
molecular
framework
might
enhance
existing
effects
perhaps
provide
entirely
Numerous
studies
shown
synergistic
additive
impact
when
fused
where
fusion
may
occur
at
coumarin-benzene
coumarin-lactone.
current
paper
explores
detail
how
linearly
ring-fused
combat
cancer.
derivative
number
42
was
determined
best
among
were
reviewed.
Compared
5-flourouracil,
IC50
values
against
six
cell
lines
promising.
These
25.08,
13.42,
41.45,
28.43,
31.15,
13.08
μM
SK-OV-3,
HeLa,
KYSE-30,
AMN3,
SKG,
MCF-7,
respectively.
attribute
obvious
compared
those
reference,
which
following
same
order
lines:
22.43,
13.37,
30.72,
24.89,
22.12,
12.42
μM.
researchers
conducted
searches
across
multiple
data
repositories,
such
Scopus,
Google
Scholar,
Web
Science,
PubMed.
After
conducting
thorough
analysis,
authors
found
included
59
pertinent
publications
published
by
end
2023.
reviewed
help
medicinal
chemists
manufacture
functionally
active
leads
using
scaffolds
been
mentioned.
knowledge
derived
offer
substantial
medical
benefits
short
term
powerful
drugs
could
boost
chemotherapeutics.
