Fluorinated indeno-quinoxaline bearing thiazole moieties as hypoglycaemic agents targeting α -amylase, and α -glucosidase: synthesis, molecular docking, and ADMET studies
Journal of Enzyme Inhibition and Medicinal Chemistry,
Год журнала:
2024,
Номер
39(1)
Опубликована: Июнь 24, 2024
Inhibition
of
α-glucosidase
and
α-amylase
are
key
tactics
for
managing
blood
glucose
levels.
Currently,
stronger,
more
accessible
inhibitors
needed
to
treat
diabetes.
Indeno[1,2-b]
quinoxalines-carrying
thiazole
hybrids
1–17
were
created
described
using
NMR.
All
analogues
tested
hypoglycaemic
effect
against
STZ-induced
diabetes
in
mice.
Compounds
4,
6,
8,
16
the
most
potent
among
synthesised
analogues.
These
examined
their
effects
on
plasma
insulin,
urea,
creatinine,
GSH,
MDA,
ALT,
AST,
total
cholesterol.
Moreover,
these
compounds
enzymes
vitro.
The
four
represented
moderate
activity
with
IC50
values
0.982
±
0.04,
10.19
0.21
inhibition
17.58
0.74
121.6
5.14
μM
when
compared
standard
medication
acarbose
IC50=0.316
0.02
31.56
1.33
inhibition.
Docking
studies
as
well
silico
ADMT
done.
Язык: Английский
The role of current synthetic and possible plant and marine phytochemical compounds in the treatment of acne
RSC Advances,
Год журнала:
2024,
Номер
14(33), С. 24287 - 24321
Опубликована: Янв. 1, 2024
Acne
is
a
long-standing
skin
condition
characterized
by
plugged
hair
follicles
due
to
the
accumulation
of
dead
cells,
sebum,
and
Propionibacterium
acnes
(
P.
)
bacteria,
causing
inflammation,
formation
pimples
or
lesions.
Язык: Английский
Fluorinated thiazole–thiosemicarbazones hybrids as potential PPAR-γ agonist and α-amylase, α-glucosidase antagonists: Design, synthesis, in silico ADMET and docking studies and hypoglycemic evaluation
Journal of Molecular Structure,
Год журнала:
2023,
Номер
1301, С. 137374 - 137374
Опубликована: Дек. 21, 2023
Язык: Английский
Unlocking the Antibacterial Potential of Naphthalimide–Coumarins to Overcome Drug Resistance with Antibiofilm and Membrane Disruption Ability against Escherichia coli
ACS Applied Materials & Interfaces,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 7, 2025
Resistance
by
bacteria
to
available
antibiotics
is
a
threat
human
health,
which
demands
the
development
of
new
antibacterial
agents.
Considering
prevailing
conditions,
we
have
developed
library
naphthalimide-coumarin
moieties
as
broad-spectrum
agents
fight
against
awful
drug
resistance.
Preliminary
studies
indicate
that
compounds
Язык: Английский
Novel Pyrrolidine-bearing quinoxaline inhibitors of DNA Gyrase, RNA polymerase and spike glycoprotein
Bioorganic Chemistry,
Год журнала:
2025,
Номер
156, С. 108218 - 108218
Опубликована: Янв. 27, 2025
Язык: Английский
Antimicrobial assessment and computational investigation of newly designed and synthesized Schiff base of chloroformylated chromene-sulfonamide derivatives against bacterial DNA gyrase
Journal of Molecular Structure,
Год журнала:
2025,
Номер
unknown, С. 142313 - 142313
Опубликована: Апрель 1, 2025
Язык: Английский
Molecular Modeling and Drug Development
Опубликована: Окт. 25, 2024
Due
to
the
utilization
of
conventional
methods
for
drug
design,
process
developing
new
drugs
has
been
rigorous
and
time-consuming.
In
silico
design
offers
a
green
way
develop
by
avoiding
many
laboratory
assays
chemicals,
which
is
an
important
extra
benefit
that
should
not
be
neglected.
The
key
in
methodologies
include
Ligand-Based
Drug
Design
(LBDD),
Structure-Based
(SBDD),
homology
modeling,
pharmacokinetics.
approach
chemicals.
This
can
help
minimize
time
cost
associated
with
development
offering
more
effective
assess
novel
before
they
are
evaluated
clinical
trials.
Язык: Английский
Discovery of Novel Bicyclic and Tricyclic Cyclohepta[b]thiophene Derivatives as Multipotent AChE and BChE Inhibitors, In-Vivo and In-Vitro Assays, ADMET and Molecular Docking Simulation
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
284, С. 117201 - 117201
Опубликована: Дек. 24, 2024
Язык: Английский