Advanced Synthesis & Catalysis,
Journal Year:
2023,
Volume and Issue:
365(18), P. 3063 - 3068
Published: March 15, 2023
Abstract
We
presented
a
cascade
transformation
of
N
,
‐diallylamines
and
fluoroalkyl
iodides
into
various
functionalized
fluoroalkylated
pyrrolidines
through
visible
light‐induced
synthetic
process
in
the
solvent‐free
conditions.
In
this
reaction
system,
substrate
N,
‐diallylamine
acted
both
as
base
electron
donor.
further
demonstrated
practicality
protocol
by
direct
modification
amino
acids
pharmaceutical
molecules.
Pharmaceutics,
Journal Year:
2023,
Volume and Issue:
15(11), P. 2554 - 2554
Published: Oct. 29, 2023
Five-membered
heterocycles
are
essential
structural
components
in
various
antibacterial
drugs;
the
physicochemical
properties
of
a
five-membered
heterocycle
can
play
crucial
role
determining
biological
activity
an
drug.
These
affect
drug’s
spectrum,
potency,
and
pharmacokinetic
toxicological
properties.
Using
scientific
databases,
we
identified
discussed
antibacterials
used
therapy,
containing
their
molecular
structure.
The
design
contain
one
to
four
heteroatoms
(nitrogen,
oxygen,
sulfur).
Antibacterials
were
discussed,
highlighting
imprinted
by
targeted
heterocycle.
In
some
antibacterials,
with
five
atoms
pharmacophores
responsible
for
specific
activity.
As
pharmacophores,
these
help
new
medicinal
molecules,
improving
potency
selectivity
comprehending
structure-activity
relationship
antibiotics.
Unfortunately,
particular
also
potential
toxicity.
review
extensively
presents
most
successful
five-atom
medicines.
Understanding
optimizing
intrinsic
characteristics
development
drugs
improved
activity,
profile,
safety.
Frontiers in Pharmacology,
Journal Year:
2023,
Volume and Issue:
14
Published: Sept. 6, 2023
To
overcome
numerous
health
disorders,
heterocyclic
structures
of
synthetic
or
natural
origin
are
utilized,
and
notably,
the
emergence
various
side
effects
existing
drugs
used
for
treatment
resistance
disease-causing
microorganisms
renders
ineffective.
Therefore,
discovery
potential
therapeutic
agents
that
utilize
different
modes
action
is
utmost
significance
to
circumvent
these
constraints.
Pyrrolidines,
pyrrolidine-alkaloids,
pyrrolidine-based
hybrid
molecules
present
in
many
products
pharmacologically
important
agents.
Their
key
roles
pharmacotherapy
make
them
a
versatile
scaffold
designing
developing
novel
biologically
active
compounds
drug
candidates.
This
review
aims
provide
an
overview
recent
advancements
(especially
during
2015-2023)
exploration
pyrrolidine
derivatives,
emphasizing
their
as
fundamental
components
skeletal
structure.
In
contrast
previous
reviews
have
predominantly
focused
on
singular
biological
activity
associated
with
molecules,
this
consolidates
findings
from
investigations
encompassing
wide
range
activities
(antimicrobial,
antiviral,
anticancer,
anti-inflammatory,
anticonvulsant,
cholinesterase
inhibition,
carbonic
anhydrase
inhibition)
exhibited
by
derivatives.
study
also
anticipated
serve
valuable
resource
research
development
endeavors,
offering
significant
insights
guidance.
European Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
275, P. 116556 - 116556
Published: June 5, 2024
Azepanes
or
azepines
are
structural
motifs
of
many
drugs,
drug
candidates
and
evaluated
lead
compounds.
Even
though
compounds
having
N-heterocyclic
7-membered
rings
often
found
in
nature
(e.g.
alkaloids),
the
natural
this
group
rather
rare
as
approved
therapeutics.
Thus,
recently
studied
azepane
azepine-congeners
predominantly
consist
semi-synthetically
synthetically-obtained
scaffolds.
In
review
a
comparison
drugs
investigated
leads
was
proposed
taking
into
regard
their
aspects
(stereochemistry),
biological
activities,
pharmacokinetic
properties
confirmed
molecular
targets.
The
N-heterocycles
reveal
wide
range
not
only
against
CNS
diseases,
but
also
e.g.
antibacterial,
anticancer,
antiviral,
antiparasitic
allergy
agents.
As
most
potential
structures,
belonging
to
N-heterocycles,
synthetic
scaffolds,
report
reveals
different
efficient
metal-free
cascade
approaches
useful
synthesize
both
simple
azepine-containing
congeners
those
oligocyclic
structures.
Stereochemistry
azepane/azepine
fused
systems,
view
data
binding
with
targets,
is
discussed.
Apart
from
we
compare
advances
SAR
studies
(mainly
2018
2023),
whereas
related
part
concerning
various
domino
strategies
focused
on
last
ten
years.
Molecules,
Journal Year:
2023,
Volume and Issue:
28(6), P. 2751 - 2751
Published: March 18, 2023
Several
nitrogen
heterocyclic
analogues
have
been
applied
to
clinical
practice,
and
about
75%
of
drugs
approved
by
the
FDA
contain
at
least
a
moiety.
Thus,
heterocycles
are
beneficial
scaffolds
that
occupy
central
position
in
development
new
drugs.
The
fact
certain
compounds
significantly
activate
NRF2/ARE
signaling
pathway
upregulate
expression
NRF2-dependent
genes,
especially
HO-1
NQO1,
underscores
need
study
roles
pharmacological
effects
N-based
moieties
NRF2
activation.
Furthermore,
exhibit
significant
antioxidant
anti-inflammatory
activities.
NRF2-activating
molecules
tremendous
research
interest
recent
times
due
their
therapeutic
neuroinflammation
oxidative
stress-mediated
diseases.
A
comprehensive
review
NRF2-inducing
activities
derivatives
will
broaden
prospects
wide
range
present
review,
as
first
its
kind,
provides
an
overview
activation
underpinning
actions
several
diseases,
properties
structural–activity
relationship
also
discussed
with
aim
making
discoveries
stimulate
innovative
this
area.
Organic Letters,
Journal Year:
2022,
Volume and Issue:
24(29), P. 5407 - 5411
Published: July 18, 2022
Herein,
a
photoinduced
palladium-catalyzed
annulation
of
1,3-dienes
with
bifunctional
halognated
alkylamines
has
been
developed,
offering
facile
route
to
access
broad
range
vinylpyrrolidines.
The
reactivity
profile
this
protocol
was
able
be
readily
manipulated
assemble
vinylpyrrolidine
and
vinlysilaazacycle.
Remarkably,
the
utility
strategy
further
illustrated
in
construction
complex
biologically
important
molecules
as
well
diversity-oriented
transformations
resulting
product.
Journal of Biomolecular Structure and Dynamics,
Journal Year:
2023,
Volume and Issue:
42(7), P. 3441 - 3458
Published: May 26, 2023
AbstractAbstractThe
synthesis
and
biological
assessment
of
novel
multi-functionalized
pyrrolidine-containing
benzenesulfonamides
were
reported
along
with
their
antimicrobial,
antifungal,
CAs
inhibition,
AChE
inhibition
as
well
DNA-binding
effects.
The
chemical
structure
the
compounds
was
elucidated
by
using
FTIR,
NMR,
HRMS.
Compound
3b,
which
had
Ki
values
17.61
±
3.58
nM
(hCA
I)
5.14
0.61
II),
found
be
most
potent
inhibitor.
Compounds
6a
6b
showed
remarkable
effects
22.34
4.53
27.21
3.96
in
comparison
to
tacrine.
6a–6c
moderate
antituberculosis
effect
on
M.
tuberculosis
a
MIC
value
15.62
μg/ml.
weaker
antifungal
antibacterial
activity
range
500–62.5
μg/ml
against
standard
bacterial
fungal
strains.
Besides
these
above,
molecular
docking
studies
performed
examine
evaluate
interaction
(3b,
6b)
current
enzymes
(CAs
AChE).
Novel
gained
interest
terms
enzyme
inhibitory
potencies.
Therefore,
inhibitors
may
considered
lead
modified
for
further
research.Communicated
Ramaswamy
H.
SarmaKeywords:
Acetylcholinesteraseantimicrobialbenzenesulfonamidecarbonic
anhydrasemolecular
dockingpyrazolepyrrolidines
Disclosure
statementNo
potential
conflict
author(s).Additional
informationFundingWe
gratefully
acknowledge
financial
support
from
Çukurova
University
(Projects
No:
TSA-2021-13814
TSA-2021-13443).Correction
StatementThis
article
has
been
corrected
minor
changes.
These
changes
do
not
impact
academic
content
article.
Molecules,
Journal Year:
2025,
Volume and Issue:
30(2), P. 394 - 394
Published: Jan. 18, 2025
Heterocyclic
compounds
represent
one
of
the
most
important
classes
natural
and
synthetic
compounds,
playing
essential
roles
in
various
fields,
including
medicinal
chemistry
[...]
