Molecules,
Journal Year:
2023,
Volume and Issue:
28(13), P. 5208 - 5208
Published: July 4, 2023
Malaria
is
one
of
the
major
life-threatening
health
problems
worldwide.
Artesunate
most
potent
antimalarial
drug
to
combat
severe
malaria.
However,
development
resistance,
short
plasma
half-life,
and
poor
bioavailability
limit
efficacy
this
drug.
Here,
we
applied
dimerization
concept
synthesize
dimeric
artesunate
glycerol
monocaprylate
conjugate
(D-AS-GC)
by
conjugating
(AS)
with
(GC)
via
esterification
reaction.
D-AS-GC
conjugate,
AS,
GC
were
well
characterized
1H
NMR,
attached
proton
test
(APT)
13C
NMR
2D
spectroscopy.
was
further
analyzed
ESI-TOF
MS.
Finally,
a
series
nanoemulsion
preconcentrate
(F1–F6)
prepared
mixing
different
ratios
oil
surfactant/cosurfactant
evaluated
after
dilution
an
aqueous
phase.
The
optimized
formulation
(F6)
exhibits
clear
hydrodynamic
diameter
dispersed
phase
determined
DLS
DOSY
morphology
droplets
F6
investigated
AFM,
which
revealed
formation
tiny
on
hydrophilic
mica
substrate.
Moreover,
using
less
polar
silicon
wafer
led
larger
spherical
core
shell-like
structure.
Overall,
rational
design
artesunate-based
could
potentially
be
used
in
more
efficient
delivery
systems.
BENTHAM SCIENCE PUBLISHERS eBooks,
Journal Year:
2023,
Volume and Issue:
unknown, P. 158 - 227
Published: March 5, 2023
Malaria
is
a
vector-borne
tropical
disease
caused
by
protozoans
belonging
to
the
genus
Plasmodium,
which
has
been
scourging
mankind
for
hundreds
of
millions
years.
Despite
masterful
progress
in
preventing
transmission
and
reducing
morbidity
fatal
outcomes,
malaria
on
rise
again.
Global
concerns
are
focused
spread
resistance
current
drugs
management
severe
or
ultimately
lethal
P.
falciparum
infection.
To
fully
exploit
potential
existing
agents
overcome
their
critical
drawbacks,
novel
synthetic
formulation
approaches
have
explored.
In
this
field,
clinical
value
natural
drug
artemisinin
(ART)
its
derivatives
firmly
established,
ART
combination
therapies
(ACTs)
recommended
as
first-line
treatment
against
infection
chloroquine-resistant
(CQR)
strains.
Over
time,
however,
options
become
inadequate,
strict
demand
new
effective
emerged.
chapter,
medicinal
chemistry
aspects
artemisinins
will
be
discussed,
covering
unique
mode
action
structural
features
relation
stability,
pharmacokinetic
profile,
antiplasmodial
activity.
Beyond
ACT
strategies,
significant
classes
compounds
obtained
through
both
covalent
bitherapy
dimerization
presented
well.
Furthermore,
special
section
focus
most
recent
endoperoxide-based
antimalarials
powerful
cost-effective
alternatives
“golden
drug”.
It
expected
that
reported
results
provide
strong
incentive
further
studies,
unceasing
research
efforts
succeed
reaching
eventual
eradication
endemic
plague.<br>
Organic Chemistry Frontiers,
Journal Year:
2024,
Volume and Issue:
11(23), P. 6768 - 6777
Published: Jan. 1, 2024
A
new
domino
approach
enables
the
simultaneous
construction
of
a
benzene
ring,
along
with
amine
and
fluorine
installation.
Resulting
ortho
-fluoroanilines
can
be
used
to
synthesize
fluorinated
azo
dye
antiviral
(tetrahydro)quinazolines.
Angewandte Chemie,
Journal Year:
2023,
Volume and Issue:
135(31)
Published: April 29, 2023
Abstract
Visible‐light‐induced
photoreaction
of
carboranes
is
an
effective
approach
to
prepare
carborane‐containing
compounds.
While
several
methods
involving
boron‐centered
carboranyl
radicals
have
been
established,
those
for
carbon‐centered
are
underdeveloped,
except
the
UV‐light‐promoted
photohomolysis.
Herein,
we
describe
a
simple
but
access
by
photoreduction
carborane
phosphonium
salts
under
blue
light
irradiation
without
using
transition
metals
and
photocatalysts.
The
utility
method
was
demonstrated
successfully
preparing
range
carborane‐oxindole‐pharmaceutical
hybrids
radical
cascade
reactions.
Computational
experimental
studies
suggest
that
generated
single‐electron
transfer
photoactive
charge‐transfer
complexes
between
additive
potassium
acetate.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(13), P. 5208 - 5208
Published: July 4, 2023
Malaria
is
one
of
the
major
life-threatening
health
problems
worldwide.
Artesunate
most
potent
antimalarial
drug
to
combat
severe
malaria.
However,
development
resistance,
short
plasma
half-life,
and
poor
bioavailability
limit
efficacy
this
drug.
Here,
we
applied
dimerization
concept
synthesize
dimeric
artesunate
glycerol
monocaprylate
conjugate
(D-AS-GC)
by
conjugating
(AS)
with
(GC)
via
esterification
reaction.
D-AS-GC
conjugate,
AS,
GC
were
well
characterized
1H
NMR,
attached
proton
test
(APT)
13C
NMR
2D
spectroscopy.
was
further
analyzed
ESI-TOF
MS.
Finally,
a
series
nanoemulsion
preconcentrate
(F1–F6)
prepared
mixing
different
ratios
oil
surfactant/cosurfactant
evaluated
after
dilution
an
aqueous
phase.
The
optimized
formulation
(F6)
exhibits
clear
hydrodynamic
diameter
dispersed
phase
determined
DLS
DOSY
morphology
droplets
F6
investigated
AFM,
which
revealed
formation
tiny
on
hydrophilic
mica
substrate.
Moreover,
using
less
polar
silicon
wafer
led
larger
spherical
core
shell-like
structure.
Overall,
rational
design
artesunate-based
could
potentially
be
used
in
more
efficient
delivery
systems.
