International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(20), P. 15120 - 15120
Published: Oct. 12, 2023
Fifty-two
kinds
of
N′-phenylhydrazides
were
successfully
designed
and
synthesized.
Their
antifungal
activity
in
vitro
against
five
strains
C.
albicans
(Candida
albicans)
was
evaluated.
All
prepared
compounds
showed
varying
degrees
their
MIC80
(the
concentration
tested
when
inhibition
rate
at
80%),
TAI
(total
index),
TSI
susceptibility
index)
calculated.
The
inhibitory
activities
27/52
fluconazole-resistant
fungi
4395
5272
much
better
than
those
fluconazole.
values
14/52
fungus
5122
less
4
μg/mL,
so
it
the
most
sensitive
(TSIB
=
12.0).
A11
best
SC5314,
4395,
(MIC80
1.9,
4.0,
3.7
μg/mL).
B14
D5
four
(2.71),
(2.13),
(2.25)
are
highest.
Further
exploration
mechanisms
revealed
that
treated
with
compound
produced
free
radicals
reactive
oxygen
species,
mycelium
morphology
damaged.
In
conclusion,
N′-phenylhydrazide
scaffold
potential
development
lead
compounds.
Among
them,
A11,
B14,
demonstrated
particularly
promising
held
as
novel
agents.
Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(24), P. 4672 - 4676
Published: Nov. 10, 2023
Abstract
2‐Iminothiazolidin‐4‐one,
5‐ethylidenethiazolidin‐4‐one,
and
thiazolidine‐4‐thione
are
all
medicinally
relevant
structures.
In
this
work,
a
NaSO
2
CF
3
‐promoted
[2+2+1]
cascade
annulation
reaction
of
‐imidoyl
sulfoxonium
ylides
isothiocyanates
was
reported
to
synthesize
variety
decorated
thiazolidine‐4‐thiones
in
35–91%
yields
with
exclusive
stereoselectivity.
The
gram‐scale
further
chemoselective
S
‐alkylations
demonstrated
the
synthetic
utilities
transformation.
Abstract
A
base‐mediated
cascade
reaction
of
CF
3
‐imidoyl
sulfoxonium
ylides
(TFISYs)
and
diimides
has
been
developed
for
the
preparation
functionalized
amidines.
In
transformation,
a
nucleophilic
addition
subsequent
[2,3]‐sigmatropic
rearrangement
ylide
occur
to
enable
an
intramolecular
migration
dimethyl
sulfoxide
(DMSO).
The
unexpected
result
protocol
demonstrates
chameleonic
reactivity
TFISYs.
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(20), P. 15120 - 15120
Published: Oct. 12, 2023
Fifty-two
kinds
of
N′-phenylhydrazides
were
successfully
designed
and
synthesized.
Their
antifungal
activity
in
vitro
against
five
strains
C.
albicans
(Candida
albicans)
was
evaluated.
All
prepared
compounds
showed
varying
degrees
their
MIC80
(the
concentration
tested
when
inhibition
rate
at
80%),
TAI
(total
index),
TSI
susceptibility
index)
calculated.
The
inhibitory
activities
27/52
fluconazole-resistant
fungi
4395
5272
much
better
than
those
fluconazole.
values
14/52
fungus
5122
less
4
μg/mL,
so
it
the
most
sensitive
(TSIB
=
12.0).
A11
best
SC5314,
4395,
(MIC80
1.9,
4.0,
3.7
μg/mL).
B14
D5
four
(2.71),
(2.13),
(2.25)
are
highest.
Further
exploration
mechanisms
revealed
that
treated
with
compound
produced
free
radicals
reactive
oxygen
species,
mycelium
morphology
damaged.
In
conclusion,
N′-phenylhydrazide
scaffold
potential
development
lead
compounds.
Among
them,
A11,
B14,
demonstrated
particularly
promising
held
as
novel
agents.
