Synthetic Communications,
Год журнала:
2024,
Номер
54(23), С. 2052 - 2063
Опубликована: Окт. 24, 2024
Herein,
we
designed
a
series
of
guanidinobenzoic
acid
ester
derivatives
on
the
basis
approved
AP
drugs,
such
as
nafamostat,
gabexate
and
camostat,
evaluated
their
inhibitory
effects
trypsin
anti-inflammatory
activity.
Among
them,
five
compounds
(6a,
6c–6e,
7j)
showed
excellent
with
IC50
values
0.0756
μM
to
0.1227
μM,
which
are
more
potent
than
nafamostat
gabexate.
Moreover,
6a,
6b
6c
also
significant
potency
against
pro-inflammatory
molecule
NO
1.618
2.276
3.022
respectively.
Consequently,
potential
lead
simultaneously
anti-trypsin
activities
were
identified,
would
profit
further
structural
optimization
for
treatment
AP.
Mini-Reviews in Medicinal Chemistry,
Год журнала:
2022,
Номер
23(4), С. 380 - 398
Опубликована: Июль 4, 2022
Alzheimer's
Disease
(AD)
is
a
common
neurodegenerative
disorder
that
almost
incurable
with
the
existing
therapeutic
interventions.
Due
to
high-risk
factors
associated
this
disease,
there
global
pursuit
of
new
anti-AD
agents.
Herein,
we
explore
biochemical
pathways
which
are
responsible
for
initiation/propagation
disease.
It
observed
out
two
isoforms
β-secretase,
β-site
amyloid
precursor
protein
cleaving
enzyme
1
(BACE1)
and
2
(BACE2)
present
in
brain,
BACE1
plays
predominant
role
commencement
AD.
Moreover,
catalytic
activities
acetylcholinesterase
butyrylcholinesterase
regulate
concentration
neurotransmitters,
they
needed
be
kept
under
control
during
signs
Hence,
these
enzymes
also
serve
as
potential
targets
treatment
AD
patients.
Keeping
view
multifactorial
nature
reviewed
multitarget
approach
tried
identify
structural
features
those
molecules
act
on
different
cellular
therapy.
Chemistry & Biodiversity,
Год журнала:
2024,
Номер
21(3)
Опубликована: Фев. 7, 2024
Three
undescribed
isosteroidal
alkaloids,
przewalskines
A-C
(1-3),
as
well
seven
known
alkaloids
(4-10)
were
obtained
from
Fritillaria
przewalskii
bulbs.
Their
structures
deduced
by
extensive
HRESIMS,
1D
NMR,
and
2D
NMR
analyses,
their
bioactivities
evaluated
involving
the
anti-inflammatory
inhibitory
potencies
on
AChE,
BChE,
Aβ
aggregation.
Compound
4
revealed
potent
effect
inhibiting
aggregation
activity
with
IC
Synthetic Communications,
Год журнала:
2024,
Номер
54(23), С. 2052 - 2063
Опубликована: Окт. 24, 2024
Herein,
we
designed
a
series
of
guanidinobenzoic
acid
ester
derivatives
on
the
basis
approved
AP
drugs,
such
as
nafamostat,
gabexate
and
camostat,
evaluated
their
inhibitory
effects
trypsin
anti-inflammatory
activity.
Among
them,
five
compounds
(6a,
6c–6e,
7j)
showed
excellent
with
IC50
values
0.0756
μM
to
0.1227
μM,
which
are
more
potent
than
nafamostat
gabexate.
Moreover,
6a,
6b
6c
also
significant
potency
against
pro-inflammatory
molecule
NO
1.618
2.276
3.022
respectively.
Consequently,
potential
lead
simultaneously
anti-trypsin
activities
were
identified,
would
profit
further
structural
optimization
for
treatment
AP.
