Results in Chemistry,
Год журнала:
2024,
Номер
7, С. 101349 - 101349
Опубликована: Янв. 1, 2024
Phospholipase
D3
(PLD3)
and
D4
(PLD4)
are
endolysosomal
exonucleases
of
ssDNA
ssRNA
that
regulate
innate
immunity.
Polymorphisms
these
enzymes
correlated
with
numerous
human
diseases,
including
Alzheimer's,
rheumatoid
arthritis,
systemic
sclerosis.
Pharmacological
modulation
immunoregulatory
proteins
may
yield
novel
immunotherapies
adjuvants.
A
previous
study
reported
a
high-throughput
screen
(N
=
17,952)
discovered
PLD3-selective
activator
inhibitor,
as
well
nonselective
but
failed
to
identify
selective
modulators
PLD4.
However,
for
PLD4
therapeutically
pertinent,
since
recent
reports
have
shown
regulating
this
protein
has
direct
implications
in
cancer
autoimmune
diseases.
Furthermore,
the
high
expression
dendritic
myeloid
cells,
comparison
broader
PLD3,
presents
opportunity
cell-targeted
immunotherapy.
Here,
we
describe
screening
an
expended
diversity
library
45,760)
improved
platform
report
discovery
one
inhibitor
three
activators
kinetic
modeling
structural
analysis
suggest
mechanistic
differences
hits.
These
findings
further
establish
utility
provide
set
chemical
scaffolds
guide
future
small-molecule
development
immunoregulator
target.
Catalysts,
Год журнала:
2023,
Номер
13(9), С. 1311 - 1311
Опубликована: Сен. 20, 2023
Terephthalohydrazide
chitosan
hydrogel
(TCs)
was
prepared
and
investigated
as
an
ecofriendly
biopolymeric
catalyst
for
synthesis
of
some
novel
thiazole
thiadiazole
derivatives.
Thus,
TCs
used
a
promising
basic
biocatalyst
preparation
three
new
series
thiazoles
two
thiadiazoles
derivatives
via
reacting
2-(2-oxo-1,2-diphenylethylidene)
hydrazine-1-carbothio-amide
with
various
hydrazonoyl
chlorides
α-haloketones
under
mild
ultrasonic
irradiation.
Also,
their
yield%
estimated
using
in
comparative
study.
The
procedure
being
employed
has
the
advantages
reaction
conditions,
quick
durations,
high
yields.
It
also
benefits
from
catalyst’s
capacity
to
be
reused
several
times
without
significantly
losing
potency.
chemical
structures
newly
compounds
were
confirmed
by
IR,
MS,
1H-NMR.
Docking
analyses
synthesized
compounds’
binding
modes
revealed
scores
against
amino
acids
selected
protein
(PDB
Code—1JIJ).
SwissADME’s
online
tool
is
then
analyze
physiochemical
pharmacokinetic
characteristics
most
significant
substances.
majority
showed
zero
violation
Lipinski’s
rule
(Ro5).
The Journal of Organic Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 7, 2025
A
novel
metal-free
[3+2]
cycloaddition
strategy
involving
(E)-β-iodovinyl
sulfones
or
bromoallylsulfones
and
pyridinium
1,4-zwitterionic
thiolates
for
the
efficient
synthesis
of
sulfonylthiophenes
is
presented.
This
method
exhibits
good
substrate
tolerance,
catalysis,
easily
prepared
bench-stable
substrates.
The
findings
highlight
a
practical
protocol
accessing
sulfonyl-substituted
thiophenes
with
significant
biological
chemical
relevance,
serving
as
an
alternative
to
traditional
metal
catalysis
oxidation
aryl/heteroaryl
sulfides.
