JAC-Antimicrobial Resistance,
Journal Year:
2024,
Volume and Issue:
7(1)
Published: Dec. 26, 2024
Ensuring
timely
and
equitable
access
to
effective
optimal
antimicrobials
is
crucial
for
patient
care,
minimize
the
use
of
less
appropriate
treatment
options
reduce
risk
antimicrobial
resistance
(AMR).
To
determine
average
time
new
antibacterials
gain
registration
in
Australia
after
obtaining
marketing
approval
internationally,
quantify
'new'
older
unregistered
Australian
clinical
practice
between
2018
2023.
Two
data
sources
were
utilized
estimate
usage
not
registered
Australia.
Annual
hospital
inpatient
sourced
from
National
Antimicrobial
Utilisation
Surveillance
Program
(NAUSP)
on
Special
Access
Scheme
(SAS)
applications
was
Government
Department
Health
Aged
Care.
Between
2023
there
36
131
unapproved
In
26.6%
cases,
an
a
critically
ill
patient.
Levofloxacin,
pyrazinamide,
tetracycline
pristinamycin
most
frequently
accessed
antimicrobials.
Applications
increased
55
249
Inpatient
nine
reported
hospitals
2023,
two
seven
unregistered.
Unapproved
are
by
clinicians
patients
unable
be
treated
with
Policy
reform
economic
incentives
required
support
needed
otherwise
untreatable
infections
ensure
sustainability
supply.
Research Square (Research Square),
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 26, 2024
Abstract
8-Nitrobenzo-1,3-thiazin-4-ones
(BTZs)
are
a
promising
class
of
antitubercular
agents
with
novel
mechanism
action,
viz.
suicide
inhibition
decaprenylphosphoryl-β-d-ribose
2’-epimerase
(DprE1),
an
enzyme
crucial
for
cell
wall
synthesis
in
the
pathogen
Mycobacterium
tuberculosis.
8-Nitro-2-(piperidin-1-yl)-6-(trifluoromethyl)-4H-benzo-1,3-thiazin-4-one
(1)
is
chemically
simplified
analogue
anti-tuberculosis
phase
2
clinical
drug
candidate
BTZ-043.
Structural
elucidation
1
solid-state
has
been
carried
out
by
X-ray
crystallography
and
two
polymorphic
forms
have
revealed.
1-I
crystallizes
triclinic
system
(space
group
P-1,
Z
=
6)
one
molecule
exhibiting
whole-molecule
disorder
preferred
orientation.
The
crystal
structure
1-II
belongs
to
tetragonal
P43,
4)
exhibits
positional
several
parts
molecule.
Applied Biosciences,
Journal Year:
2024,
Volume and Issue:
3(4), P. 468 - 483
Published: Oct. 21, 2024
This
study
explores
the
interaction
between
Vemurafenib
(VEM),
a
potent
BRAF
inhibitor,
and
calf
thymus
DNA
(ctDNA)
using
comprehensive
array
of
biophysical
computational
techniques.
The
primary
objective
is
to
understand
potential
off-target
effects
VEM
on
DNA,
given
its
established
role
in
melanoma
therapy
targeting
V600E
mutation.
investigation
employed
methods
such
as
ultraviolet–visible
absorption
spectroscopy,
steady-state
fluorescence,
circular
dichroism,
isothermal
titration
calorimetry,
advanced
molecular
dynamics
simulations.
results
indicate
that
interacts
with
primarily
through
minor
groove-binding
mechanism,
causing
minimal
structural
disruption
double
helix.
Viscosity
measurements
melting
temperature
analyses
further
confirmed
this
non-intercalative
mode
binding.
Calorimetry
data
revealed
an
exothermic,
thermodynamically
favorable
ctDNA,
driven
by
both
enthalpic
entropic
factors.
Finally,
computer
simulations
identified
most
probable
binding
site
within
groove
nucleic
acid,
providing
basis
for
experimental
findings.
Antibiotics,
Journal Year:
2024,
Volume and Issue:
13(10), P. 992 - 992
Published: Oct. 19, 2024
In
the
present
study,
a
series
of
isatin
bis-imidathiazole
hybrids
was
designed
and
synthesized
to
develop
new
class
heterocyclic
compounds
with
improved
antimicrobial
activity
against
pathogens
responsible
for
hospital-
community-acquired
infections.
A
remarkable
inhibitory
ChemistrySelect,
Journal Year:
2024,
Volume and Issue:
9(43)
Published: Nov. 1, 2024
Abstract
Benzothiazinone
analogs
have
emerged
as
a
promising
class
of
compounds
having
potent
antimycobacterial
activity,
particularly
against
Mycobacterium
tuberculosis
,
the
pathogen
responsible
for
tuberculosis.
This
review
highlights
development
benzothiazinone
potential
antitubercular
agents
from
beginning
to
recent
advancement
in
past
decade.
These
shown
including
drug‐resistant
strains
.
Structure–activity
relationship
studies
and
modifications
improved
their
efficacy.
favorable
pharmacokinetic
profiles
show
promise
preclinical
studies.
Challenges
include
addressing
resistance
mechanisms
ensuring
safety.
Their
unique
mode
action
properties
make
them
attractive
candidates
battle
Pharmaceutics,
Journal Year:
2024,
Volume and Issue:
16(12), P. 1490 - 1490
Published: Nov. 21, 2024
Background/Objectives:
The
aims
of
this
work
were
to
formulate
cannabidiol
in
different
lipid
carriers
for
skin
delivery
after
topical
application
and
study
their
stability,
interaction
with
the
skin,
antibacterial
activity.
Methods:
Solid
nanoparticles
nanostructured
loaded
prepared
characterized
terms
physicochemical
properties,
colloidal
protection
antioxidant
capacity
cannabidiol,
as
well
retention
over
time.
Skin
penetration
was
assessed
using
an
vitro
model
human
skin.
activity
tested
against
Staphylococcus
aureus
compared
free
cannabidiol.
Results:
Three
nanoformulations
exhibited
best
size
reproducibility
values
selected
further
studies.
formulations
stable,
protected
active
ingredient,
succeeded
delivering
it
deep
layers,
demonstrated
Conclusions:
These
show
potential
use
diseases
conditions,
they
protect
enhance
its
exhibit
effects.
Russian Journal of Oncology,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 6, 2024
BACKGROUND:
New
opportunities
for
the
treatment
of
malignant
tumors,
including
those
resistant
to
conventional
drugs,
are
opening
up
with
development
new
antitumor
drugs
based
on
benzimidazoles.
Benzimidazole
compounds
have
a
wide
range
biological
activities,
anticancer
activity.
Benzimidazoles
exhibit
significant
cytotoxicity
against
number
human
tumor
cell
lines.
The
study
effects
synthetic
benzimidazole
derivatives
growth
models
in
vivo
will
allow
effective
doses
and
regimens
cancer
such
compounds.
AIM:
To
investigate
effect
bis-benzimidazole
monomeric
compound
MB2Py(Ac)
dimeric
DB2Py(3).
transplantable
Lewis
lung
carcinoma
(LLC)
B16
melanoma
mice.
METHODS:
In
were
evaluated
transplanted
by
single
intravenous
administration
Irinotecan
was
used
as
comparison
drug.
Standard
indices
inhibition
(TPO%)
index
(TGI)
evaluate
activity
investigated.
RESULTS:
DB2Py(3)
MB2Py(Ac),
at
schedules
tested,
showed
weak
murine
solid
(TPO
50%).
model,
maximum
15%
38.5%,
respectively.
LLC
weak,
reaching
only
8%
23.4%
control
drug
irinotecan
more
pronounced
but
short,
TPO
52.5%
34.5%
cancer.
Overall,
sensitive
bis-benzimidazoles
than
CONCLUSIONS:
that
among
tested
models,
most
promising.
However,
its
high
toxicity
requires
further
optimization
clinical
use.
proved
be
least
effective,
can
also
investigated
modified
forms.
JAC-Antimicrobial Resistance,
Journal Year:
2024,
Volume and Issue:
7(1)
Published: Dec. 26, 2024
Ensuring
timely
and
equitable
access
to
effective
optimal
antimicrobials
is
crucial
for
patient
care,
minimize
the
use
of
less
appropriate
treatment
options
reduce
risk
antimicrobial
resistance
(AMR).
To
determine
average
time
new
antibacterials
gain
registration
in
Australia
after
obtaining
marketing
approval
internationally,
quantify
'new'
older
unregistered
Australian
clinical
practice
between
2018
2023.
Two
data
sources
were
utilized
estimate
usage
not
registered
Australia.
Annual
hospital
inpatient
sourced
from
National
Antimicrobial
Utilisation
Surveillance
Program
(NAUSP)
on
Special
Access
Scheme
(SAS)
applications
was
Government
Department
Health
Aged
Care.
Between
2023
there
36
131
unapproved
In
26.6%
cases,
an
a
critically
ill
patient.
Levofloxacin,
pyrazinamide,
tetracycline
pristinamycin
most
frequently
accessed
antimicrobials.
Applications
increased
55
249
Inpatient
nine
reported
hospitals
2023,
two
seven
unregistered.
Unapproved
are
by
clinicians
patients
unable
be
treated
with
Policy
reform
economic
incentives
required
support
needed
otherwise
untreatable
infections
ensure
sustainability
supply.
