Journal of Medicinal Chemistry,
Journal Year:
2022,
Volume and Issue:
65(5), P. 3962 - 3977
Published: Feb. 23, 2022
Bioisosteric
H/F
or
CH2OH/CF2H
replacement
was
introduced
in
coumarin
derivatives
previously
characterized
as
dual
AChE-MAO
B
inhibitors
to
probe
the
effects
on
both
inhibitory
potency
and
drug-likeness.
Along
with
vitro
screening,
we
investigated
early-ADME
parameters
related
solubility
lipophilicity
(Sol7.4,
CHI7.4,
log
D7.4),
oral
bioavailability
central
nervous
system
(CNS)
penetration
(PAMPA-HDM
PAMPA-blood-brain
barrier
(BBB)
assays,
Caco-2
bidirectional
transport
study),
metabolic
liability
(half-lives
clearance
microsomes,
inhibition
of
CYP3A4).
Both
specific
nonspecific
tissue
toxicities
were
determined
SH-SY5Y
HepG2
lines,
respectively.
Compound
15
bearing
a
-CF2H
motif
emerged
water-soluble,
orally
bioavailable
CNS-permeant
potent
inhibitor
human
AChE
(IC50
=
550
nM)
MAO
8.2
nM,
B/A
selectivity
>
1200).
Moreover,
behaved
safe
metabolically
stable
neuroprotective
agent,
devoid
cytochrome
liability.
Oxidative Medicine and Cellular Longevity,
Journal Year:
2021,
Volume and Issue:
2021(1)
Published: Jan. 1, 2021
Coumarins
belong
to
the
benzopyrone
family
commonly
found
in
many
medicinal
plants.
Natural
coumarins
demonstrated
a
wide
spectrum
of
pharmacological
activities,
including
anti‐inflammatory,
anticoagulant,
anticancer,
antibacterial,
antimalarial,
casein
kinase‐2
(CK2)
inhibitory,
antifungal,
antiviral,
Alzheimer’s
disease
inhibition,
neuroprotective,
anticonvulsant,
phytoalexins,
ulcerogenic,
and
antihypertensive.
There
are
very
few
studies
on
bioavailability
coumarins;
therefore,
further
investigations
necessitated
study
different
which
already
showed
good
biological
activities
previous
studies.
On
evidence
varied
properties,
present
work
presents
an
overall
review
derivation,
availability,
capacities
with
consideration
essential
mode
their
therapeutic
actions.
In
conclusion,
variety
available,
current
interest
thanks
synthetic
accessibility
riches
perform
valuable
function
as
agents
range
medical
fields.
Molecules,
Journal Year:
2021,
Volume and Issue:
26(2), P. 501 - 501
Published: Jan. 19, 2021
Coumarins
are
naturally
occurring
molecules
with
a
versatile
range
of
activities.
Their
structural
and
physicochemical
characteristics
make
them
privileged
scaffold
in
medicinal
chemistry
chemical
biology.
Many
research
articles
reviews
compile
information
on
this
important
family
compounds.
In
overview,
the
most
recent
papers
from
2020
organized
analyzed,
discussion
these
data
is
included.
Multiple
electronic
databases
were
scanned,
including
SciFinder,
Mendeley,
PubMed,
latter
being
main
source
information.
Particular
attention
was
paid
to
potential
coumarins
as
an
drug
design,
well
fluorescent
probes
for
decaging
prodrugs,
metal
detection,
diagnostic
purposes.
Herein
we
do
analysis
trending
topics
related
coumarin
its
derivatives
broad
field
discovery.
RSC Medicinal Chemistry,
Journal Year:
2023,
Volume and Issue:
15(1), P. 10 - 54
Published: Oct. 20, 2023
Many
researchers
around
the
world
are
working
on
development
of
novel
anticancer
drugs
with
different
mechanisms
action.
In
this
case,
coumarin
is
a
highly
promising
pharmacophore
for
drugs.
Besides,
hybridization
moiety
other
pharmacophores
has
emerged
as
potent
breakthrough
in
treatment
cancer
to
decrease
its
side
effects
and
increase
efficiency.
This
review
aims
provide
comprehensive
overview
recent
derivatives
their
application
Herein,
we
highlight
describe
largest
number
research
works
reported
field
from
2015
August
2023,
along
action
structure-activity
relationship
studies,
making
articles
published
topic
date.
Chemistry & Biodiversity,
Journal Year:
2024,
Volume and Issue:
21(5)
Published: March 20, 2024
Abstract
Fruits
and
vegetables
serve
not
only
as
sources
of
nutrition
but
also
medicinal
agents
for
the
treatment
diverse
diseases
maladies.
These
dietary
components
are
significant
resources
phytochemicals
that
demonstrate
therapeutic
properties
against
many
illnesses.
Fraxin
is
a
naturally
occurring
coumarin
glycoside
mainly
present
in
various
species
Fraxinus
genera,
having
multitude
uses
disorders.
This
study
focuses
to
investigate
pharmacological
activities,
botanical
sources,
biopharmaceutical
profile
phytochemical
fraxin
based
on
different
preclinical
non‐clinical
studies
show
scientific
evidence
evaluate
underlying
molecular
mechanisms
effects
ailments.
For
this,
data
was
searched
collected
(as
February
15,
2024)
variety
credible
electronic
databases,
including
PubMed/Medline,
Scopus,
Springer
Link,
ScienceDirect,
Wiley
Online,
Web
Science,
Google
Scholar.
The
findings
demonstrated
favorable
outcomes
relation
range
or
medical
conditions,
inflammation,
neurodegenerative
disorders
such
cerebral
ischemia‐reperfusion
(I/R)
depression,
viral
infection,
well
diabetic
nephropathy.
showed
protective
osteoprotective,
renoprotective,
pulmoprotective,
hepatoprotective,
gastroprotective
due
its
antioxidant
capacity.
has
great
capability
diminish
oxidative
stress‐related
damage
organs
by
stimulating
enzymes,
downregulating
nuclear
factor
kappa
B
NLRP3,
triggering
Nrf2/ARE
signaling
pathways.
exhibited
poor
oral
bioavailability
because
reduced
absorption
wide
distribution
into
tissues
organs.
However,
extensive
research
required
decipher
profiles,
clinical
necessary
establish
efficacy
natural
compound
reliable
agent.
Frontiers in Pharmacology,
Journal Year:
2021,
Volume and Issue:
12
Published: June 11, 2021
Lung
cancer
is
the
most
common
malignancy
and
leads
to
around
one-quarter
of
all
deaths.
Great
advances
have
been
achieved
in
treatment
lung
with
novel
anticancer
agents
improved
technology.
However,
morbidity
mortality
rates
remain
extremely
high,
calling
for
an
urgent
need
develop
anti-lung
agents.
1,2,3-Triazole
could
be
readily
interact
diverse
enzymes
receptors
organisms
through
weak
interaction.
can
not
only
acted
as
a
linker
tether
different
pharmacophores
but
also
serve
pharmacophore.
This
review
aims
summarize
recent
1,2,3-triazole-containing
compounds
potential,
their
structure-activity
relationship
(SAR)
together
mechanisms
action
discussed
pave
way
further
rational
development
candidates.
