Synthesis of new pyridine-thiazolidin-4-one and pyridine-pyrazole-thiazolidin-4-one conjugates: Molecular modelling and docking as antimicrobial agents
Journal of Molecular Structure,
Год журнала:
2024,
Номер
1309, С. 138233 - 138233
Опубликована: Апрель 3, 2024
Язык: Английский
New Hybrids of Thiazole Clubbed with Fluorinated Benzene: Design, Synthesis, Spectral, Antimicrobial, and Molecular Docking Studies
Journal of Molecular Structure,
Год журнала:
2025,
Номер
unknown, С. 141670 - 141670
Опубликована: Фев. 1, 2025
Язык: Английский
Synthesis of Amide Core Based New 5‐methyl‐2‐(2H‐1,2,3‐triazol‐2‐yl)benzamide Scaffolds As Antifungal, Antimicrobial Agents, and Molecular Docking Study
ChemistrySelect,
Год журнала:
2025,
Номер
10(15)
Опубликована: Апрель 1, 2025
Abstract
A
new
series
of
5‐methyl‐2‐(2
H
‐1,2,3‐triazol‐2‐yl)benzamide
was
successfully
designed
and
synthesized
by
acid
amine
coupling
reaction
5‐methyl‐2‐(2H‐1,2,3‐triazol‐2‐yl)benzoic
different
types
aliphatic
aromatic
amines.
The
compounds
were
characterized
1
NMR,
13
C
FT‐IR
mass
spectra.
scaffolds
(H1‐H20)
evaluated
for
its
antifungal
antibacterial
activity
in
vitro
against
C.
albicans
(Candida
albicans),
A.
clavatus
(Aspergillus
clavatus),
niger
Niger),
E.
coli
(Escherichia
coli),
P.
aeruginosa
(Pseudomonas
Aeruginosa),
S.
aureus
(Staphylococcus
Aureus)
,
pyogenes
(Streptococcus
Pyogenus)
.
Compounds
H3
H7
H9
H13
H14
H17
H19
most
effective
(
MIC
250
µg/mL
)
compared
to
standard
drug
griseofulvin
500
).
all
1,2,3‐triazoles
good
moderate
ciprofloxacin
chloramphenicol
drugs.
Moreover,
silico
molecular
docking
study,
the
with
highest
potential
examine.
result
showed
strong
receptor
site
binding
affinity
indicated
promising
potential.
Язык: Английский
Insight into the therapeutic potential of pyrazole‐thiazole hybrids: A comprehensive review
Archiv der Pharmazie,
Год журнала:
2024,
Номер
unknown
Опубликована: Окт. 4, 2024
Abstract
Several
pyrazole‐thiazole
hybrids
featuring
two
potentially
bioactive
pharmacophores
with
or
without
linker
have
been
synthesized
using
the
molecular
hybridization
approach
as
target
structures
by
medicinal
chemists
to
modulate
multiple
drug
targets
simultaneously.
The
presented
review
aims
provide
an
overview
of
diversified
and
wide
array
pharmacological
activities
these
bestowing
anticancer,
antifungal,
antibacterial,
analgesic,
anti‐inflammatory,
antioxidant,
antitubercular,
antiviral,
antiparasitic,
miscellaneous
activities.
structure–activity
relationships
potential
mechanism
action
are
also
reviewed
shed
light
on
development
more
effective
biotargeted
candidates.
This
focuses
latest
research
advances
in
biological
profile
reported
from
2015
present,
providing
researchers
a
comprehensive
platform
rationally
design
develop
promising
hybrids.
Язык: Английский
Synthesis and biological evaluation of novel D-ring fused steroidal N(2)-substituted-1,2,3-triazoles
RSC Medicinal Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
In
this
study,
a
series
of
13
new
D-ring
fused
steroidal
N
(2)-substituted-1,2,3-triazoles
were
synthesized,
characterized
and
evaluated
for
their
biological
activities.
Язык: Английский
Theoretical and Pharmacological Investigations of Phenylthiazol-2, 4 Dihydroxybenzaldehyde Condensed Schiff Base
Biomedical & Pharmacology Journal,
Год журнала:
2024,
Номер
17(4), С. 2535 - 2549
Опубликована: Дек. 30, 2024
The
ability
of
thiazole
derivatives
to
alter
the
activity
numerous
metabolic
enzymes
suggests
that
they
have
promising
therapeutic
applications.
Their
antimicrobial,
antifungal,
anti-inflammatory,
antioxidant,
and
antiproliferative
properties
were
also
established.
Schiff
base,
which
was
formed
by
combining
2,
4-dihydrxy
benzaldehyde
with
phenyl
amine,
studied
using
UV,
FTIR,
1H,
13C-NMR.
significant
absorption
(283
nm)
vibrational
peaks
at
1625
cm-1
observed
for
imine
group.
compound
confirmed
presence
a
free
proton
carbon
peak
following
aromatic
peaks.
derivative
underwent
theoretical
biological
evaluations,
such
as
antibacterial,
inhibition
alpha
amylase,
DPPH
scavenging
assays.
Using
an
online
server,
QSAR
parameters
predicted
synthesised
molecule
compared
drug
likeness
Lipinski
five
rules.
experimental
results
are
DFT
docking
outcomes.
revealed
compound's
reactivity
decreased
hardness
feature.
Docking
interaction
score
ranges
from
-5.2
-11.2
kcal/mol.
antimicrobial
against
pathogens
Acinetobacter
baumannii,
Methicillin-resistant
Staphylococcus
aureus,
aureus
between
12
15
mm
zone
minimum
concentration
maximum
150±0.28
µg/mL.
Likely,
antidiabetic
antioxidant
outcomes
showed
effective
428.73±0.32
590.36±
0.34
There
excellent
agreement
values
in
prepared
base.
Язык: Английский