Abstract
Here
we
present
the
synthesis
of
a
new
fluorinated
pyridyl‐azo
dye
and
demonstrate
an
effective
way
to
convert
monomer
H‐aggregated
form
through
UV‐light
induced
trans‐cis‐trans
photoisomerization.
And
upto
12
:
88
ratio
between
aggregation
was
achieved
small
pulse
UV
irradiation.
The
H‐aggregation
shows
unique
high
extinction
co‐efficient
in
UV‐visible
absorbance
unexpected
fluorescence
emission
with
remarkably
large
Stokes
shift.
solvent
DMF
fluorine
substituent
were
found
have
critical
role
aggregation.
1
H,
19
F
NMR,
F‐DOSY
NMR
experiments
used
confirm
also
absence
π‐π
stacking.
Polymers,
Год журнала:
2024,
Номер
16(6), С. 843 - 843
Опубликована: Март 19, 2024
Chemotherapy
together
with
surgery
and/or
radiotherapy
are
the
most
common
therapeutic
methods
for
treating
cancer.
However,
off-target
effects
of
chemotherapy
known
to
produce
side
and
dose-limiting
toxicities.
Novel
delivery
platforms
based
on
natural
synthetic
polymers
enhanced
pharmacokinetic
potential
treatment
cancer
have
grown
tremendously
over
past
10
years.
Polymers
can
facilitate
selective
targeting,
enhance
prolong
circulation,
improve
delivery,
provide
controlled
release
cargos
through
various
mechanisms,
including
physical
adsorption,
chemical
conjugation,
internal
loading.
Notably,
that
biodegradable,
biocompatible,
physicochemically
stable
considered
be
ideal
carriers.
This
biomimetic
bio-inspired
system
offers
a
bright
future
effective
drug
overcome
obstacles
encountered.
review
focuses
barriers
impact
success
as
well
recent
developments
improving
Chemical Science,
Год журнала:
2024,
Номер
15(8), С. 2712 - 2724
Опубликована: Янв. 1, 2024
Frustrated
Lewis
pair
(FLP)
bond
activation
chemistry
has
greatly
developed
over
the
last
two
decades
since
seminal
report
of
metal-free
reversible
hydrogen
activation.
Recently,
FLP
systems
have
been
utilized
to
allow
monoselective
C-F
(at
equivalent
sites)
in
polyfluoroalkanes.
The
problem
'over-defluorination'
functionalization
polyfluoroalkanes
(where
multiple
fluoro-positions
are
uncontrollably
functionalized)
a
long-standing
chemical
fluorocarbon
for
80
years.
mediated
is
complementary
other
solutions
address
and
offers
several
advantages
unique
opportunities.
This
perspective
highlights
some
these
opportunities
places
development
into
context
wider
effort
overcome
'over-defluorination'.
Pharmaceuticals,
Год журнала:
2024,
Номер
17(3), С. 281 - 281
Опубликована: Фев. 22, 2024
The
fluorine
atom
possesses
many
intrinsic
properties
that
can
be
beneficial
when
incorporated
into
small
molecules.
These
include
the
atom’s
size,
electronegativity,
and
ability
to
block
metabolic
oxidation
sites.
Substituents
feature
fluorine-containing
groups
are
currently
prevalent
in
drugs
lower
cholesterol,
relieve
asthma,
treat
anxiety
disorders,
as
well
improve
chemical
of
various
medications
imaging
agents.
dye
scaffolds
(fluorescein/rhodamine,
coumarin,
BODIPY,
carbocyanine,
squaraine
dyes)
reported
will
address
incorporation
scaffold
contribution
it
provides
its
application
an
agent.
It
is
also
important
recognize
radiolabeled
atoms
used
for
PET
early
detection
diseases.
This
review
discuss
benefits
incorporating
molecules
give
examples
fluorinated
pharmaceutical
industry
techniques.
Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 7, 2025
Transient
receptor
potential
canonical
channels
4
and
5
(TRPC4/5)
are
nonselective
cation
involved
in
emotional
regulation,
positioning
them
to
be
promising
targets
for
treating
mental
disorders
such
as
anxiety
depression.
HC-070,
a
potent
TRPC4/5
inhibitor,
exhibits
significant
anxiolytic
antidepressant
effects
animal
models,
though
its
drug-like
properties
require
optimization.
In
this
study,
we
applied
property-based
drug
design
(PBDD)
approach
optimize
leading
the
discovery
of
compound
32,
which
shows
improved
LipE
Fsp3
values,
reduced
hERG
blocking
activity,
enhanced
metabolic
stability,
increased
aqueous
solubility,
superior
oral
bioavailability.
Oral
administration
32
mouse
models
demonstrates
efficacy
comparable
fluoxetine.
This
study
supports
therapeutic
inhibitors
identifies
candidate
further
investigation.
Furthermore,
our
work
underscores
value
PBDD
optimizing
lead
compounds
during
process.
ACS Omega,
Год журнала:
2024,
Номер
9(26), С. 28129 - 28143
Опубликована: Июнь 19, 2024
An
efficient
and
mild
protocol
for
the
visible
light-induced
radical
cascade
difluoromethylation/cyclization
of
imidazoles
with
unactivated
alkenes
using
easily
accessible
bench-stable
difluoromethyltriphenylphosphonium
bromide
as
precursor
-CF
Abstract
Hydroxy
azo‐benzenes
are
very
well
known
for
their
rapid
trans
⇆
cis
photoisomerization
under
polar
solvents.
In
contrast,
we
synthesized
two
hydroxymethylated‐
hydroxyazobenzene
derivatives
and
investigated
light‐triggered
stability
The
result
showed
just
opposite
behavior
slow
isomerization
was
observed
(minutes‐days).
Thus,
the
UV‐vis
spectrum
revealed
a
low
decrease
in
absorbance
of
π–π*
transition.
Surprisingly,
process
became
faster
with
addition
ionic
species.
Here,
attempted
to
understand
underlying
cause
unusual
photo‐switching
behavior.
presence
hydroxymethyl
fluorine
substituents
found
have
significant
effect
on
photo‐isomerized
products.
it
confirmed
NMR
DLS
studies
that
photostability
compounds
caused
by
solvent‐assisted
aggregation
(hydrodynamic
radius,
R
H
5660–1720
nm)
which
underwent
dispersion
(R
H,
220–68
formed
stable
solvated
photoproduct
photoirradiation.
Furthermore,
this
aggregation‐dispersion
be
slowly
reversible.
Further,
fluorescence
emission
demonstrated
characteristic
dispersion‐induced
quenching.
Regular
photoswitching
non‐polar
conditions
benzene
where
an
expected
blue
shift
transition
increase
intensity
n–π*
transitions.
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(7), С. 5391 - 5420
Опубликована: Фев. 14, 2024
This
study
aimed
to
develop
novel
rapid-acting
antidepressants
with
sustained
efficacy
and
favorable
safety
profiles.
We
designed
synthesized
a
series
of
fluorine-containing
scopolamine
analogues
evaluated
their
antidepressant
potential.
In
vitro
cytotoxicity
assays
showed
that
most
these
compounds
exhibited
minimal
toxicity
against
neuronal
non-neuronal
mammalian
cell
lines
(IC50
>
100
μM).
The
activities
the
were
using
tail
suspension
test,
S-3a
was
identified
as
lead
compound
potent
effects.
Behaviorally,
alleviated
depressive
symptoms
in
mice
displayed
higher
cognitive
margin
than
scopolamine.
Toxicological
assessments
confirmed
S-3a's
safety,
while
pharmacokinetics
rapid
clearance
(half-life:
16.6
min).
Mechanistically,
antagonized
M1
receptors
elevated
BDNF
levels,
suggesting
its
potential
an
for
further
exploration.
The Journal of General Physiology,
Год журнала:
2025,
Номер
157(4)
Опубликована: Апрель 28, 2025
Voltage-gated
sodium
channels
underpin
electrical
signaling
in
sensory
neurons.
Their
activity
is
an
essential
element
the
vast
majority
of
pain
conditions,
making
them
significant
drug
targets.
Sensory
neuron
play
roles
not
only
afferent
but
also
a
range
efferent
regulatory
mechanisms.
Side
effects
through
actions
on
other
cell
types
and
are
thus
important
issues
to
address
during
analgesic
development.
As
example,
human
genetic
evidence
for
NaV1.7
as
ideal
target
contrasts
with
side
antagonists.
In
this
review,
we
describe
history
progress
toward
development
useful
drugs
renewed
focus
NaV1.8
key
treatment.
antagonists
alone
or
combination
analgesics
likely
provide
new
opportunities
relief
number
people
(about
33%
population)
impacted
by
chronic
pain,
particularly
present
aging
populations.
