Synthesis and Medicinal Impacts of Novel 3,3′-Bihalocoumarins and Their Precursors, 7-Halocoumarin-3-acetic Acids
Russian Journal of Bioorganic Chemistry,
Год журнала:
2025,
Номер
51(2), С. 802 - 815
Опубликована: Апрель 1, 2025
Язык: Английский
Synthesis of Eugenol-Derived Coumarins as Broad-Spectrum Biosafe Antimicrobial Agents
Russian Journal of Bioorganic Chemistry,
Год журнала:
2024,
Номер
50(6), С. 2240 - 2251
Опубликована: Дек. 1, 2024
Язык: Английский
None
Journal of Medicinal and Chemical Sciences,
Год журнала:
2022,
Номер
5(6)
Опубликована: Июнь 12, 2022
The
majority
of
the
world’s
most
hazardous
pathologies
are
linked
to
oxidative
damaging
effect
free
moieties.
One
diseases
associated
with
these
radicals
is
diabetes.
This
disease
widely
distributed
among
people
all
ages,
elderly
being
affected.
Therefore,
it
essential
conduct
comprehensive
investigations
in
order
promote
creation
novel
radical-housing
and
hypoglycemic
compounds.
study
involves
synthesis
eight
albocarbon-based
coumarins,
which
were
confirmed
by
various
spectrophotometers.
Their
effects
analyzed.
pharmacokinetic
profile
was
checked
silico
using
pre-ADMET,
known
as
a
online
program.
influence
tested
against
two
types
blood
glucose-controlling
enzymes.
In
addition,
new
compounds’
potency
index
measured.
potential
analyzed
testing
coumarins’
ability
scavenge
DDPT
hydroxyl
harmful
radicals.
Pharmacokinetic
studies
demonstrated
that
synthesized
coumarins
penetrate
gastrointestinal
mucosa
very
well,
compounds
blood-brain
barrier
only
slightly.
These
findings
suggest
good
oral
bioavailability
along
low
neurological
toxicity
profiles.
investigation
revealed
they
had
less
potent
enzyme
inhibition
capacity
compared
standard,
LY5
powerful
one.
Besides,
assessment
also
indicated
them
active
than
reference.
Among
them,
LY0
strongest
compound
from
recognitions,
safety
parameters
accordance
computer-based
study.
researchers
believed
can
be
applied
for
successful
drugs
help
modulation
much
serious
pathology.
Язык: Английский
None
Journal of Medicinal and Chemical Sciences,
Год журнала:
2022,
Номер
6(7)
Опубликована: Дек. 24, 2022
Dipeptidyl
peptidase
4
(DPP-4)
inhibition
is
a
promising
therapy
for
type
2
diabetes.
Inhibition
of
DPP-4
limits
the
breakdown
glucagon-like
peptide
1
(GLP-1),
hence
increasing
functional
GLP-1
levels.
This
boosts
secretion
insulin
and
decreases
glucagon
release,
resulting
in
reduction
blood
sugar
In
an
effort
to
discover
chemical
structural
prerequisite
inhibition,
computational
investigations
involving
Quantitative
Structural–Activity
Relationship
(QSAR)
studies
were
performed
on
63
compounds
with
pIC50
values
ranging
from
7.0
9.744.
With
good
R2
(0.716)
cross-validated
correlation
coefficient
value
Q2
LOO
(0.6120),
model
was
created
that
quantitatively
describes
relationship.
The
regression
approach
systematically
gives
topological
state
atom,
presence
CF3
at
second
position
triazole
ring
(knotpv),
polarizabilities
(RDF15p),
atomic
masses
(MATS3M),
heteroatom,
valence
distribution
had
significant
effect
(Chiv4pc).
addition,
docking
results
revealed
favorable
contacts
between
triazolopiperazine
analogues
catalytically
amino
acid
residues,
including
HIS740,
SER630,
ASN710,
GLU205.
Comparing
interactions
most
active
compound
those
standard
Sitagliptin
reveals
comparable
binding
energies.
study
demonstrates
substituting
nucleus
incorporating
polarity-altering
groups
are
advantageous
inhibiting
enzyme.
Язык: Английский