New thiazole derivatives linked to pyridine, fused pyridine, pyrimidine and thiazolopyrimidine scaffolds with potential dual anticancer and antimicrobial activities: Design, synthesis and docking simulation
Journal of Molecular Structure,
Год журнала:
2024,
Номер
1316, С. 138973 - 138973
Опубликована: Июнь 11, 2024
Язык: Английский
Bioactive Fused Pyrazoles Inspired by the Adaptability of 5-Aminopyrazole Derivatives: Recent Review
Molecules,
Год журнала:
2025,
Номер
30(2), С. 366 - 366
Опубликована: Янв. 17, 2025
Heterocyclic
compounds,
especially
those
containing
the
pyrazole
moiety,
are
highly
significant
in
organic
chemistry
and
possess
remarkable
diverse
biological
properties.
The
5-aminopyrazole
derivatives
key
starting
materials
for
synthesis
of
numerous
bioactive
compounds
such
as
pyrazolopyridine,
pyrazolopyrimidine,
pyrazoloquinazoline,
pyrazolotriazine
derivatives.
Many
inspired
by
a
wide
spectrum
activities
medicinal
applications
antioxidants,
anticancer
agents,
enzyme
inhibitors,
antimicrobials,
anti-tuberculosis
activities.
This
review
summarizes
recently
reported
methods
fused
pyrazole-based
based
on
within
last
5
years
(2020
to
present).
One
important
goals
this
is
illustrate
future
strategies
design,
development,
utilization
products
potent
drugs.
Язык: Английский
Pyrazole-thiazole hybrids: Synthesis, computational studies and impact on digestive enzymes
Journal of Molecular Structure,
Год журнала:
2024,
Номер
1316, С. 138847 - 138847
Опубликована: Июнь 3, 2024
Язык: Английский
Evaluation of the Antihypoxic Effect of Methyl 6-Aryl-5-Aroyl-4-Hydroxy(Methoxy)-2-Oxo(Thioxo)-Hexahydropyrimidine-4-Carboxylates
Pharmaceutical Chemistry Journal,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 22, 2025
Язык: Английский
Recent advancements of pyrimidine chemistry thriving deeper into drug discovery
Synthetic Communications,
Год журнала:
2025,
Номер
unknown, С. 1 - 29
Опубликована: Апрель 3, 2025
Язык: Английский
A versatile precursor for one‐pot synthesis of novel azo‐thiazole and thiazole scaffolds as prospective antimicrobial and antioxidant agents
Journal of the Chinese Chemical Society,
Год журнала:
2024,
Номер
71(10), С. 1309 - 1323
Опубликована: Авг. 2, 2024
Abstract
In
this
study,
we
present
a
simple
method
for
preparing
new
series
of
thiazoles
with
excellent
isolated
yields.
To
synthesize
the
target
thiazole
scaffolds,
straightforward
one‐pot
procedure
was
developed
including
an
amine‐mediated
reaction
isoxazolethiazolidin‐4‐one
derivative,
thiosemicarbazide,
and
appropriate
hydrazonyl
chlorides.
The
conditions
protocol
were
optimized
by
experimenting
different
solvents
amines.
best
results
achieved
conducting
in
dioxane
triethylamine
at
100°C
5
h.
structures
desired
products
proved
elemental
analyses
spectral
data.
Additionally,
antimicrobial
efficacy
all
derivatives
assessed
against
various
types
microorganisms.
observed
indicated
that
activity
thiosemicarbazone
derivative
2
strongest
among
series,
MIC
values
ranging
from
0.03
±
0.01
to
0.98
0.15
μg/mL.
Moreover,
antioxidant
evaluations
conducted
on
targets,
using
ascorbic
acid
as
reference
drug.
Significantly,
10
demonstrated
most
promising
inhibitory
effects.
further
toxicity
studies
performed
active
novel
compounds,
revealing
their
drug‐like
properties
varying
risks
humans.
Язык: Английский
Antibacterial and Antifungal Pyrazoles Based on Different Construction Strategies
Muneeb Ur Rehman,
Fang He,
Xi Shu
и другие.
European Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
282, С. 117081 - 117081
Опубликована: Ноя. 20, 2024
Язык: Английский
New Quinazolin-4(3H)-One Derivatives Incorporating Isoxazole Moiety as Antioxidant Agents: Synthesis, Structural Characterization, and Theoretical DFT Mechanistic Study
Pharmaceuticals,
Год журнала:
2024,
Номер
17(10), С. 1390 - 1390
Опубликована: Окт. 18, 2024
Background:
This
research
centers
on
the
development
and
spectroscopic
characterization
of
new
quinazolin-4(3H)-one-isoxazole
derivatives
(5a–e).
The
aim
was
to
investigate
regioselectivity
1,3-dipolar
cycloaddition
involving
arylnitriloxides
N-propargylquinazolin-4(3H)-one,
assess
antioxidant
properties
synthesized
compounds.
synthetic
approach
started
with
alkylation
quinazolin-4(3H)-one
using
propargyl
bromide,
followed
by
a
reaction.
Methods:
structural
identification
products
performed
various
methods,
such
as
IR,
1H,
13C,
HMBC
NMR,
HRMS,
single-crystal
X-ray
diffraction.
To
further
examine
cycloaddition,
Density
Functional
Theory
(DFT)
calculations
at
B3LYP/6-31G(d)
level
were
employed.
Additionally,
potential
compounds
tested
in
vitro
DPPH
(2,2-Diphenyl-1-picrylhydrazyl)radical
scavenging
assays.
reaction
selectively
produced
3,5-disubstituted
isoxazoles,
regiochemical
outcome
being
independent
substituents
phenyl
ring.
Results:
Theoretical
DFT
agreement
experimental
results,
revealing
activation
energies
−81.15
kcal/mol
for
P-1
−77.32
P-2,
favoring
formation
P-1.
An
analysis
Intrinsic
Reaction
Coordinate
(IRC)
confirmed
that
proceeded
via
concerted
but
asynchronous
mechanism.
tests
demonstrated
exhibited
significant
radical
activity,
shown
assay.
N-propargylquinazolin-4(3H)-one
successfully
resulted
novel
isoxazoles.
Conclusions:
findings
well-supported
theoretical
predictions,
assays
revealed
strong
indicating
future
biological
applications
these
Язык: Английский
One-pot synthesis of new benzo[4,5]imidazo[1,2- a ]pyrimidines and pyrazolo[1,5- a ] pyrimidines as an eco-friendly and effective method catalyzed by acetic acid with prospective antimicrobial agents
Synthetic Communications,
Год журнала:
2024,
Номер
unknown, С. 1 - 14
Опубликована: Окт. 28, 2024
Язык: Английский
A Greener Process for the Synthesis of Base‐Catalyzed Substituted Pyrazoles and Triazolopyrimidines as Prospective Biological Activity
ChemistrySelect,
Год журнала:
2024,
Номер
9(48)
Опубликована: Дек. 1, 2024
Abstract
Novel
1
H
‐pyrazole
analogues
were
generated
in
high
yields
via
the
cyclocondensation
of
chalcone
derivatives
with
p‐toluene
sulfonyl
hydrazine,
utilizing
K
2
CO
3
and
iodine
as
catalysts
under
heat
for
h.
A
straightforward
effective
manner
was
carried
out
creation
substituted
pyrazoles
or
triazolopyrimidines
tandem
methods
containing
aryl
sulfonyl/benzoyl
chloride
derivatives,
chalcones
5‐aminotriazole,
catalytic
amounts
KOH,
respectively.
By
researching
different
solvents
catalysts,
reaction
conditions
this
technique
improved,
resulting
good
to
excellent
intended
products
4aa‐cb
6A‐d
.
This
method
is
observed
its
enhanced
environmental
friendliness.
The
structures
novel
molecules
have
been
verified
by
spectroscopic
elemental
analysis
techniques.
targets
validated
versus
various
pathogenic
fungal
strains.
Contrasting
new
series
reference
drugs,
pyrazole
derivative
2b
strongest
antimicrobial
actions,
MIC
values
varying
from
0.98–19.45
µM.
Язык: Английский