Triazination/IEDDA Cascade Modular Strategy Installing Pyridines/Pyrimidines onto Tyrosine Enables Peptide Screening and Optimization
Journal of the American Chemical Society,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 30, 2025
Modular
chemical
postmodification
of
peptides
is
a
promising
strategy
that
supports
the
optimization
and
innovation
hit
peptide
therapeutics
by
enabling
rapid
derivatization.
However,
current
methods
are
primarily
limited
to
traditional
bio-orthogonal
strategies
ligation
techniques,
which
require
preintroduction
non-natural
amino
acids
impose
fixed
limit
diversity.
Here,
we
developed
Tyrosine-1,2,3-Triazine
Ligation
(YTL)
strategy,
constructs
novel
linkages
(pyridine
pyrimidine)
through
"one-pot,
two-step"
process
combining
SNAr
IEDDA
reactions,
promoting
modular
post
modification
Tyr-containing
peptides.
After
optimizing
YTL
establishing
standard
procedures,
successfully
applied
it
solid-phase
various
biorelated
peptides,
such
as
synthesis
dual-mode
imaging
probes
long-acting
GLP-1
analogs.
As
proof
concept,
library
384
amphipathic
was
constructed
using
based
on
96-well
microfiltration
plates.
modifications
were
then
performed
screened
template
tripeptide
RYR,
leading
generation
20
derivatives.
The
antibacterial
activity
these
derivatives
systematically
characterized,
identifying
Z8
potential
candidate.
Язык: Английский
The Liebeskind–Srogl Cross-Coupling Reaction Towards the Synthesis of Biologically Active Compounds
European Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown, С. 117526 - 117526
Опубликована: Март 1, 2025
Язык: Английский
Ionic Liquid-Assisted Approaches in the Synthesis of Nitrogen-Containing Heterocycles: A Focus on 3- to 6-Membered Rings
Journal of Ionic Liquids,
Год журнала:
2025,
Номер
unknown, С. 100146 - 100146
Опубликована: Март 1, 2025
Язык: Английский
Iodine-Catalyzed Room-Temperature Aerobic Oxidation of C(sp3)–H Bonds and Its Application in the Synthesis of Quinoxaline Derivatives
The Journal of Organic Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 1, 2025
An
iodine-catalyzed
aerobic
oxidation
reaction
of
C(sp3)-H
bonds
was
established
at
room
temperature.
In
this
transformation,
iodine
acts
as
a
Lewis
acid
catalyst,
and
the
pyridine
moiety
in
substrate
plays
crucial
role.
Under
optimum
conditions,
picolyl
ketone
substrates
were
smoothly
transformed
into
corresponding
1,2-dicarbonyl
compounds,
subsequent
introduction
1,2-diaminobenzenes
mixture
led
to
formation
various
quinoxaline
derivatives.
This
synthetic
process
does
not
use
transition
metals
also
features
mild
operational
simplicity,
gram-scale
synthesis.
Язык: Английский
Design and Synthesis of New Pyridine-Thiazole Hybrids as Potential Antibacterial Agents: Spectral, Antimicrobial, and in silico Molecular Docking Studies
Journal of Molecular Structure,
Год журнала:
2025,
Номер
unknown, С. 142612 - 142612
Опубликована: Май 1, 2025
Язык: Английский
Unraveling Structural and Anticancer Properties of Pyridine-Oxadiazole Derivatives: Single-Crystal XRD, Hirshfeld Analysis, and Cytotoxicity against A549 Cells
ACS Omega,
Год журнала:
2025,
Номер
unknown
Опубликована: Июнь 1, 2025
Язык: Английский
CYP3A4 drug metabolism considerations in pediatric pharmacotherapy
Medicinal Chemistry Research,
Год журнала:
2024,
Номер
unknown
Опубликована: Дек. 5, 2024
Abstract
Cytochrome
P450
3A4
(CYP3A4)
is
a
crucial
enzyme
involved
in
the
Phase
I
metabolism
of
numerous
medications
used
clinical
practice.
Its
potential
significance
pediatric
pharmacotherapy
underscored
by
unique
metabolic
profile
children,
which
differs
markedly
from
adults,
especially
neonates,
infants,
and
young
children
due
to
developmental
changes
activity.
This
review
explores
critical
role
CYP3A4
drugs
population,
with
particular
focus
on
combination
drug
therapies.
Given
high
for
drug-drug
interactions
therapies,
understanding
modulation
activity
essential
optimizing
therapeutic
outcomes
minimizing
adverse
effects.
paper
further
examines
structural
similarities
between
these
bergamottin,
known
inhibitor
found
citric
fruits
such
as
grapefruit.
Variability
activity,
influenced
genetic
polymorphisms,
stage,
external
factors,
necessitates
careful
consideration
prescribing
management
children.
corroborates
need
personalized
medicine
approaches
enhanced
pharmacovigilance
ensure
safe
effective
use
CYP3A4-metabolized
population.
Graphical
Язык: Английский