Synthesis and Activity of Novel Pyrazole/Pyrrole Carboxamides Containing a Dinitrogen Six-Membered Heterocyclic as Succinate Dehydrogenase and Ergosterol Biosynthesis Inhibitors against Colletotrichum camelliae
Journal of Agricultural and Food Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 23, 2025
Pyrazole
carboxamide
derivatives
were
initially
extensively
studied
as
succinate
dehydrogenase
inhibitors
(SDHIs).
In
the
present
study,
a
series
of
pyrazole/pyrrole
carboxamides
containing
dinitrogen
six-membered
heterocyclic
designed
based
on
our
reported
active
skeletons
with
dual
mode
action.
Bioactivity
results
showed
that
target
compound
Q18
demonstrated
superior
antifungal
efficacy
against
Colletotrichum
camelliae
(C.
camelliae)
an
EC50
value
6.0
mg/L.
The
in
vivo
protective
activity
was
74.7%
at
100
Scanning
electron
microscopy
and
transmission
could
disrupt
surface
morphology
mycelia
cause
lipid
peroxidation
cell
membrane,
which
further
verified
by
determination
relative
conductivity
malondialdehyde
contents.
Combined
ergosterol
content,
docking
between
SDH
CYP51,
IC50
for
(9.7
mg/L),
it
is
concluded
potential
SDHI
biosynthesis
inhibitor.
Thus,
study
provides
fresh
insight
into
amides.
Язык: Английский
Monoterpene amino alcohols in multicomponent synthesis of chiral hetero- and carbocycles
Mendeleev Communications,
Год журнала:
2025,
Номер
35(4), С. 464 - 466
Опубликована: Янв. 1, 2025
Язык: Английский
Schinus terebinthifolius essential oil and its major component delta-3-carene induce antinociception mediated by serotonergic receptors
Gabriel Carvalho de Souza Santana,
María Jesús,
Anna Beatriz Oliveira Cruz
и другие.
Journal of Ethnopharmacology,
Год журнала:
2025,
Номер
unknown, С. 120021 - 120021
Опубликована: Май 1, 2025
Язык: Английский
Synthesis, Antifungal Activity, and Molecular Simulation Study of L–Carvone‐Derived 1,3,4‐Oxadiazole‐Thioether Compounds
Rongzhu Wen,
Wengui Duan,
Guishan Lin
и другие.
Chemistry & Biodiversity,
Год журнала:
2023,
Номер
20(7)
Опубликована: Июнь 29, 2023
Abstract
To
discover
potent
antifungal
molecules
with
new
and
distinctive
structures,
20
novel
L‐carvone‐derived
1,3,4‐oxadiazole‐thioether
compounds
5
a
–
t
were
synthesized
through
multi‐step
reaction
of
L
‐
carvone,
their
structures
confirmed
by
FT‐IR,
1
H‐NMR,
13
C‐NMR,
HR‐MS.
The
activities
preliminarily
tested
in
vitro
method,
the
results
indicated
that
all
title
displayed
certain
against
eight
plant
fungi,
especially
for
P.
piricola
.
Among
them,
compound
i
(R=
p‐
F)
most
significant
activity
deserved
further
study
discovering
developing
natural
product‐based
agents.
Moreover,
two
molecular
simulation
technologies
employed
investigation
structure–activity
relationships
(SARs).
Firstly,
reasonable
effective
3D‐QSAR
model
was
established
comparative
field
(CoMFA)
relationship
substituents
linked
benzene
rings
inhibitory
elucidated.
Then,
binding
mode
its
potential
biological
target
(CYP51)
simulated
docking,
it
found
could
readily
bind
CYP51
active
site,
ligand‐receptor
interactions
involved
three
hydrogen
bonds
several
hydrophobic
effects.
Язык: Английский