Novel Hydrazide Hydrazone Derivatives as Antimicrobial Agents: Design, Synthesis, and Molecular Dynamics
Processes,
Journal Year:
2024,
Volume and Issue:
12(6), P. 1055 - 1055
Published: May 22, 2024
Ester
2
was
produced
by
reacting
thiourea
derivative
1
with
ethyl
2-chloro-3-oxobutanoate
in
MeOH
containing
piperidine.
Hydrazide
3
the
latter
ester
hydrazine
hydrate
EtOH
at
reflux.
By
hydrazide
aromatic/heterocyclic
aldehydes,
twelve
derivatives
of
hydrazone
5a–l
were
produced.
Spectral
measurements
and
elemental
analysis
verified
molecular
structure.
Compounds
2,
5a,
5c,
5d,
5f
had
strong
effects
on
all
pathogenic
bacterial
strains
according
to
an
evaluation
antimicrobial
qualities
synthetic
compounds.
With
inhibitory
zone
diameters
ranging
from
16
20.4
mm,
exhibited
strongest
activity.
Additionally,
minimum
concentration
(MIC)
assessed.
The
best
outcomes
found
hydrazones
5c
5f.
For
B.
subtilis,
MIC
2.5
mg/mL.
E.
coli
K.
pneumoniae,
mechanics-generalized
born
surface
area
(MM/GBSA)
utilized
compute
binding
free
energies
via
a
dynamics
simulation
most
active
compounds,
5c.
Moreover,
computational
analyses
demonstrated
that
substantial
affinity
for
site
DNA
gyrase
B,
suggesting
this
compound
could
be
platform
new
structure-based
design
efforts.
Language: Английский
An insight into Synthetic, Structural and Medicinal perspective of imidazole analogs: A review
Govind Yadav,
No information about this author
Ranjana Jain
No information about this author
European Journal of Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown, P. 117524 - 117524
Published: March 1, 2025
Language: Английский
Identification of hydroxyphenyl cyanovinyl thiazoles as new structural scaffold of potential antibacterial agents
Lu Xing,
No information about this author
Shaolin Zhang,
No information about this author
Cheng‐He Zhou
No information about this author
et al.
Bioorganic & Medicinal Chemistry Letters,
Journal Year:
2025,
Volume and Issue:
unknown, P. 130258 - 130258
Published: April 1, 2025
Language: Английский
Pharmaceutical perspectives of thiazole analogues: An overview
Results in Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown, P. 101820 - 101820
Published: Oct. 1, 2024
Language: Английский
One-pot, three-component synthesis and in vitro anti-bacterial evaluation of some novel chromeno[4,3-d]pyrimidine, thiazol-2H-chromens, and thiadiazol-2H-chromen derivatives
Behjat Pouramiri,
No information about this author
Maryam Sharifi,
No information about this author
Fatemeh Riyahi Zaniani
No information about this author
et al.
Journal of Molecular Structure,
Journal Year:
2025,
Volume and Issue:
unknown, P. 141658 - 141658
Published: Feb. 1, 2025
Language: Английский
Synthesis and Crystal Structural Analysis of bismuth phosphovanadate compounds: An Eco-Friendly and Recyclable Catalyst for Green Synthesis of Imidazole Derivatives
Soumya Ferraa,
No information about this author
Youssef Merroun,
No information about this author
Hanane Barebita
No information about this author
et al.
Journal of the Indian Chemical Society,
Journal Year:
2024,
Volume and Issue:
101(10), P. 101313 - 101313
Published: Aug. 18, 2024
Language: Английский
Green One-Pot Synthesis of Thiazole Scaffolds Catalyzed by Reusable NiFe2O4 Nanoparticles: In Silico Binding Affinity and In Vitro Anticancer Activity Studies
Satish Gudala,
No information about this author
Archi Sharma,
No information about this author
Aruna Lankada
No information about this author
et al.
ACS Omega,
Journal Year:
2024,
Volume and Issue:
9(36), P. 38262 - 38271
Published: Aug. 29, 2024
A
facile,
green,
one-pot
multicomponent
synthesis
strategy
was
employed
to
fabricate
novel
thiazole
scaffolds
incorporating
phthalazine,
pyridazine,
and
pyrido-pyridazine
derivatives
(4a–4o).
This
synthetic
route
entailed
the
reaction
of
an
α-halo
carbonyl
compound
(1)
with
thiosemicarbazide
(2)
various
anhydrides
(3a–3o),
utilizing
NiFe2O4
nanoparticles
as
a
reusable
catalyst
in
ethanol:water
(1:1)
solvent
system.
The
cytotoxicity
synthesized
compounds
meticulously
assessed
against
three
cancer
cell
lines,
A375,
HeLa,
MCF-7,
employing
IC50
values
(μM)
benchmark,
compared
reference
drug
erlotinib.
Compound
4n
displayed
remarkable
efficacy
A375
(0.87
±
0.31
μM),
HeLa
(1.38
1.24
MCF-7
(1.13
0.96
μM)
significantly
surpassing
erlotinib's
values.
Additionally,
4k,
4l,
4m,
4o
demonstrated
notable
across
all
tested
indicating
their
potential
effective
anticancer
agents.
In
silico
docking
studies
Hsp82
Hsp90
proteins
indicated
that
ligands
4c,
4j,
4o,
4l
had
superior
binding
affinities
ADME
analysis
showed
4n,
favorable
pharmacokinetic
profiles,
including
nontoxicity,
high
human
intestinal
absorption,
low
CYP
inhibitory
promiscuity.
Structure–activity
relationship
revealed
cyano
benzylidene
substitutions
enhanced
activity.
Overall,
compounds,
particularly
efficacy,
interactions,
promising
making
them
strong
candidates
for
further
development
Language: Английский
Synthesis of Difuropyridines from Chitin‐Derived 3‐Acetamidofuran and their Application to Photocatalytic Reactions
Advanced Synthesis & Catalysis,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 18, 2024
Abstract
Difuropyridines
have
been
prepared
from
aldehydes
and
chitin‐derived
3‐acetamidofuran
(3AF)
under
acid‐catalyzed
conditions.
were
comprehensively
synthesized
for
the
first
time.
The
difuropyridines
can
be
applied
to
prepare
fluorescent
probe
analogs
or
catalyze
decarboxylative
reactions
as
photocatalysts.
Language: Английский