Synthetic aspects, structural insights and pharmacological potential of pyrazole derivatives: an overview
Deleted Journal,
Journal Year:
2025,
Volume and Issue:
7(2)
Published: Feb. 13, 2025
Abstract
There
is
an
increase
in
infectious
diseases
every
year.
Heterocyclic
compounds
have
been
use
as
drugs
for
a
long
time.
Amongst
many
heterocyclic
derivatives,
the
containing
pyrazole
core
has
limelight
because
of
its
relative
ease
synthesis
and
excellent
biological
activities.
Pyrazoles
are
aromatic
consisting
ring
structure
where
two
nitrogen
atoms
adjacent
to
each
other
contain
three
carbon
atoms.
Over
years
pyrazoles
explored
variety
pharmacological
applications.
Herein,
this
review
overviews
information
related
industrially
important
pyrazoline
scaffolds
their
applications,
recent
literature
on
synthesizing
providing
explanation
activity
by
focusing
structural
relationship
hence
affording
ideas
design
scaffolds.
Graphical
abstract
Language: Английский
A review of recent advances in anticancer activity and SAR of pyrazole derivatives
Archiv der Pharmazie,
Journal Year:
2025,
Volume and Issue:
358(3)
Published: March 1, 2025
Abstract
The
present
review
serves
to
highlight
the
antitumor
worth
of
pyrazole
derivatives.
Several
active
pyrazole‐based
anticancer
compounds
proposed
by
a
huge
number
scientists
worldwide
are
reported.
Regarding
development
novel
agents
at
faster
tone,
there
is
need
correlate
latest
information
with
previously
available
understand
situation
this
moiety
in
drug
discovery
studies.
Herein,
different
pyrazoles
classified
according
their
mode
action
targets.
results
provided
evidence
that
derivatives
have
potential
applications
for
treatment
variety
tumor
types.
From
study's
findings,
structure–activity
relationship
(SAR)
demonstrated
all
containing
substituted
represent
an
important
scaffold
activities.
Publications
area
increasing,
and
therefore,
new
therapeutic
involving
members
could
be
discovered
near
future,
as
many
prospects
not
been
sufficiently
studied
so
far
other
In
words,
provides
overview
state
knowledge
about
structural
characteristics
most
recent
SAR
various
This
will
allow
medicinal
chemists
identify
promising
structures
guide
design
synthesis
more
effective
safer
candidates.
Language: Английский
Pyrazoles: A Master Key to Tackle Multidrug‐Resistant Acinetobacter baumannii and Its Structure Activity Relationship Studies
Saraswati Sharma,
No information about this author
S. Krishnam Raju,
No information about this author
Santosh Kumar Verma
No information about this author
et al.
Chemical Biology & Drug Design,
Journal Year:
2025,
Volume and Issue:
105(3)
Published: March 1, 2025
Infections
caused
by
Gram-negative
bacteria
within
the
ESKAPE
group
pose
significant
treatment
challenges.
These
feature
effective
efflux
pumps
and
possess
lipopolysaccharides
in
their
outer
membranes,
as
well
a
thin
peptidoglycan
layer
measuring
5-10
nm
thickness.
Acinetobacter
baumannii
(A.
baumannii),
bacterium,
is
contributor
to
serious
infections
acquired
hospitals
communities,
representing
substantial
risk
human
health.
This
bacterium
has
developed
resistance
nearly
all
existing
antibiotics,
past
50
years,
no
new
antibacterial
class
been
introduced
for
treating
A.
infections,
highlighting
an
urgent
necessity
development
of
antibacterials.
The
unique
structural
framework
adaptable
features
pyrazole
ring
attract
researchers
develop
antibiotics.
present
study
outlines
advancements
made
over
last
decade
pyrazole-containing
derivatives
that
exhibit
wide
range
activity
against
various
bacterial
strains.
Specifically,
we
discuss
effectiveness
diverse
multidrug-resistant
strains
explore
aspects
structure-activity
relationship
(SAR).
compilation
data
could
serve
excellent
platform
designing
developing
pyrazole-based
small
molecules
target
growth
baumannii.
Language: Английский
Phenol (bio)isosteres in drug design and development
Archiv der Pharmazie,
Journal Year:
2024,
Volume and Issue:
358(1)
Published: Nov. 24, 2024
Abstract
Due
to
their
versatile
properties,
phenolic
compounds
are
integral
various
biologically
active
molecules,
including
many
pharmaceuticals.
However,
application
in
drug
design
is
often
hindered
by
issues
such
as
poor
oral
bioavailability,
rapid
metabolism,
and
potential
toxicity.
This
review
explores
the
use
of
phenol
bioisosteres–structurally
similar
that
can
mimic
biological
activity
phenols
while
potentially
offering
improved
drug‐like
properties.
We
provide
an
extensive
analysis
bioisosteres,
benzimidazolones,
benzoxazolones,
indoles,
quinolinones,
pyridones,
highlighting
impact
on
pharmacokinetic
pharmacodynamic
profiles
drugs.
Case
studies
illustrate
successful
these
bioisosteres
enhancing
metabolic
stability,
receptor
selectivity,
overall
therapeutic
efficacy.
Additionally,
addresses
challenges
associated
with
bioisosterism,
maintaining
potency
avoiding
undesirable
side
effects.
By
a
detailed
examination
current
strategies
future
directions,
this
serves
valuable
resource
for
medicinal
chemists
seeking
optimize
scaffolds
development.
The
insights
provided
herein
aim
facilitate
more
effective
safer
agents
through
strategic
bioisosteric
modifications.
Language: Английский