RSC Advances,
Journal Year:
2025,
Volume and Issue:
15(2), P. 1447 - 1489
Published: Jan. 1, 2025
We
have
reviewed
the
recently
reported
multicomponent
reactions
(MCRs)
yielding
cyclic
frameworks
in
a
single
pot
from
simple
building
blocks
under
mild
conditions.
These
MCRs
may
prove
to
be
useful
for
drug
discovery
projects.
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(1), P. 125 - 125
Published: Jan. 17, 2025
Background/Objectives:
Leishmaniasis
is
one
of
the
20
Neglected
Tropical
Diseases
according
to
WHO,
affecting
approximately
12
million
people
in
four
continents,
generating
serious
public
health
problems.
The
lack
therapeutic
options,
associated
with
toxicity
and
emergence
resistance
few
available
drugs,
makes
it
urgent
develop
new
drug
options.
In
this
context,
aims
work
are
expand
knowledge
about
pharmacophore
group
responsible
for
antileishmanial
potential
2-aminothiophene
derivatives.
Thus,
compounds
were
synthesized
containing
chemical
modifications
at
C-3,
C-4,
C-5
positions
ring,
addition
S-Se
bioisosterism.
Methods:
Dozens
2-AT
2-aminoselenophen
(2-AS)
derivatives
sequentially
through
applications
Gewald
reaction
then
evaluated
vitro
their
activities
against
L.
amazonensis
cytotoxicity
macrophages.
Results:
Several
series
synthesized,
was
possible
identify
some
substitution
patterns
favorable
activity
IC50
values
below
10
µM,
such
as
non-essentiality
presence
a
carbonitrile
C-3;
importance
size
cycloalkyl/piperidinyl
chains
C-4
modulating
activity;
increase
without
safety
S/Se
bioisosteric
substitution.
Conclusions:
Taken
together,
these
findings
reaffirm
great
2-aminothiophenes
generate
candidates
offers
contributions
design
an
even
more
promising
profile
problem
leishmaniasis.
Organic Letters,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 3, 2025
We
present
an
efficient
silver-catalyzed
one-pot
controllable
molecular
editing
protocol
for
the
transformation
of
2-amino-N-substituted
benzamides
into
6-selenylated
N-substituted
1,2,3-benzotriazine-4(3H)-ones
under
mild
reaction
conditions.
This
three-component
strategy
is
achieved
by
building
N-N/N═N/C-Se
bonds,
which
provides
a
practical
pathway
preparation
selenylated
with
broad
substrate
scope
and
good
functional
group
tolerance,
as
well
high
site-selectivity.
Mechanistic
experiments
suggest
that
this
proceeds
via
intermolecular
site-selective
C-H
selenylation
readily
available
diselenides,
followed
annulation
using
AgNO3
nitrogen
synthon.
The Journal of Organic Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: March 12, 2025
Organoselenium
compounds
and
quinolines
are
widely
used
in
drugs
materials.
Herein,
we
report
an
electro-oxidative
cyclization
between
isocyanides
diselenides
to
effectively
synthesize
2-organoselenyl
a
simple
undivided
cell
without
transition-metal
catalysts
or
toxic
oxidants.
Gram-scale
synthesis
postsynthetic
modifications
highlighted
the
practicality
of
this
electrochemical
strategy.
A
series
produced
with
up
82%
yield,
good
functional
group
tolerance
high
atom
efficiency
under
room
temperature.
Oriental Journal Of Chemistry,
Journal Year:
2025,
Volume and Issue:
41(2)
Published: April 28, 2025
In
this
study,
we
disclose
the
synthesis
of
a
new
organoselenium
(OSe)
candidate,
N-phenyl-2-((4-(3-phenylthioureido)phenyl)selanyl)acetamide
(5),
achieved
in
three
synthetic
steps
starting
from
commercially
available
chemical,
aniline.
The
chemical
structure
target
OSe
compound
5
was
characterised
using
NMR,
IR,
and
mass
spectrometry.
DFT
calculations
were
performed.
results
reveal
that
1
demonstrates
lowest
HOMO
energy
(-5.03
eV)
most
significant
gap
(3.62
eV),
indicating
high
stability
low
reactivity.
contrast,
2
shows
highest
(-3.62
smallest
(1.31
confirming
its
reactivity
stability.
HB168
3
demonstrate
intermediate
properties
with
moderate
Dipole
Moment
analysis
highlights
strong
polarity
(6.47
Debye)
weak
S2
(0.27
Debye).
Additionally,
displays
electronegativity
(3.22
electrophilicity
index
(2.86
further
supporting
Conversely,
exhibits
(6.71
electrophilic
character.
prepared
docked
against
bacterial
strain
protein
targets:
Escherichia
coli
(ID:
5L3J)
as
gram-negative
bacteria,
whereas
Bacillus
Subtilis
7S3L)
Staphylococcus
aureus
3BL6)
chosen
gram-positive
bacteria.
Also,
molecular
docking
performed
drugs
reference
drug
Ampicillin
wide
spectrum
antibiotic
Ebselen,
Diphenyl
diselenide
Selenium
containing
drugs.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(44), P. 31990 - 32000
Published: Jan. 1, 2024
Inflammation
is
a
complex
process
with
many
contributing
factors,
and
it
often
causes
pain.
The
pathophysiology
of
pain
involves
the
release
inflammatory
mediators
that
initiate
sensation,
as
well
edema
other
inflammation
hallmarks.
Selenium-containing
compounds
(OSe)
are
very
promising
for
developing
new
medicines
because
they
can
treat
different
diseases.
In
this
study,
we
estimated
anti-inflammatory
properties
maleanilic
succinanilic
acids
containing
selenium
(OSe).
These
molecules
were
designed
by
combining
strategies
to
enhance
their
properties.
Hence,
impacts
8,
9,
10,
11
pursued
using
markers
COX-2,
IL-1β,
IL-6.
Notably,
was
revealed
downregulated
IL-6
(2.01,
1.63,
2.26,
2.05),
(1.42,
1.64,
1.93,
2.59),
(1.67,
2.54,
2.22,
4.06)-fold
changes,
respectively.
Moreover,
molecular
docking
studies
conducted
on
pursue
binding
affinities
COX-2
enzyme.
scores
towards
site
receptor
attained.
Additionally,
more
accurate
dynamics
simulations
performed
200
ns
docked
complexes
confirm
findings,
which
ignore
protein's
flexibility.
Therefore,
exact
stability
