IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENIY KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA,
Journal Year:
2023,
Volume and Issue:
unknown, P. 20 - 27
Published: Jan. 1, 2023
Конденсацией
полиолов
(1,2-пропандиола,
3-хлор-1,2-пропандиола
и
глицерина)
с
карбонильными
соединениями
(метилэтилкетоном
метилизобутилкетоном)
синтезированы
в
условиях
микроволнового
излучения
2,2,4-тризамещенные
1,3-диоксоланы:
2-этил-2,4-диметил-,
2-метил-2-этил-4-хлорметил-,
2-метил-2-этил-4-гидроксиметил-,
2-изобутил-2,4-диметил-,
2-метил-2-изобутил-4-хлорметил-
2-метил-2-изобутил-4-гидроксиметил-1,3-диоксоланы.
Установлено,
что
при
микроволновом
нагреве
время
синтеза
сократилось
3
раза,
этом
выход
селективность
остались
прежними
(≥
90%).
Методами
ЯМР-спектроскопии
хромато-масс-спектрометрии
подробно
изучены
структуры
полученных
соединений.
В
случае
различных
заместителей
(этильного
изобутильного)
С2
углеродном
атоме
цикла
для
молекул
1,3-диоксоланов
спектрах
1Н
13С
ЯМР
каждого
вещества
наблюдается
удвоенный
набор
сигналов
одинаковой
интенсивности,
свидетельствует
об
образовании
диастереомерных
пар
–
син-
анти-диастереомеров
соотношении
1:1.
Изучено
оценено
влияние
типа
положения
заместителя
на
физико-химические
характеристики
фрагментацию
ионы
синтезированных
веществ.
Определено,
направление
распада
2,2,4-тризамещенных
обусловлено
элиминированием
из
молекулярного
иона
радикалов
замеcтителей
СН3,
R1
и/или
R2
цикле.
соединений
антикоагуляционную
антиагрегационную
активности
in
vitro.
Найдено,
среди
синтезируемого
ряда
максимальное
значение
агрегацию
тромбоцитов
плазменное
звено
гемостаза
оказывают
хлориды
производные
2-метил-2-этил-4-хлормети-1,3-диоксолан
2-метил-изобутил-4-хлорметил-1,3-диоксолан.
Все
синтезируемые
соединения
вызывали
гипокоагуляцию,
повышая
АПТВ
(активированное
парциальное
тромбопластиновое
время)
6,2
12,4%
по
сравнению
контролем
(гепарин
натрия)
не
влияли
концентрацию
фибриногена
протрамбиновое
время.
Journal of Agricultural and Food Chemistry,
Journal Year:
2022,
Volume and Issue:
70(40), P. 12819 - 12829
Published: Sept. 29, 2022
Transketolase
(TK)
was
identified
as
a
new
target
for
the
development
of
novel
herbicides.
In
this
study,
series
naphthalimide-aroyl
hybrids
were
designed
and
prepared
based
on
TK
tested
their
herbicidal
activities.
vitro
bioassay
showed
that
compounds
4c
4w
exhibited
stronger
inhibitory
effects
against
Digitaria
sanguinalis
(DS)
Amaranthus
retroflexus
(AR)
with
inhibition
over
90%
at
200
mg/L
around
80%
100
mg/L.
Also,
excellent
postemergence
activity
DS
AR
90
g
[active
ingredient
(ai)]/ha
50
(ai)/ha
in
greenhouse,
which
comparable
mesotrione.
The
fluorescent
quenching
experiments
At
revealed
occurrence
electron
transfer
from
compound
to
formation
strong
exciplex
between
them.
Molecular
docking
analyses
further
profound
affinity
through
interaction
amino
acids
active
site,
results
its
activities
TK.
These
findings
demonstrated
is
potentially
lead
candidate
herbicides
targeting
Molecules,
Journal Year:
2023,
Volume and Issue:
28(8), P. 3373 - 3373
Published: April 11, 2023
A
series
of
new
fluorinated
quinoline
analogs
were
synthesized
using
Tebufloquin
as
the
lead
compound,
2-fluoroaniline,
ethyl
2-methylacetoacetate,
and
substituted
benzoic
acid
raw
materials.
Their
structures
confirmed
by
1H
NMR,
13C
HRMS.
The
compound
8-fluoro-2,3-dimethylquinolin-4-yl
4-(tert-butyl)benzoate
(2b)
was
further
determined
X-ray
single-crystal
diffraction.
antifungal
activity
tested
at
50
μg/mL,
bioassay
results
showed
that
these
derivatives
had
good
activity.
Among
them,
compounds
2b,
2e,
2f,
2k,
2n
exhibited
(>80%)
against
S.
sclerotiorum,
2g
displayed
(80.8%)
R.
solani.
Journal of Agricultural and Food Chemistry,
Journal Year:
2024,
Volume and Issue:
72(45), P. 25034 - 25044
Published: Nov. 5, 2024
A
series
of
myricetin
derivatives
containing
diisopropanolamine
were
designed
and
synthesized.
The
in
vitro
inhibitory
effects
the
target
compounds
on
9
fungal
pathogens
3
bacterial
also
evaluated.
A12
had
best
effect
against
Xanthomonas
oryzae
pv.
(Xoo),
with
an
EC50
value
4.9
μg/mL,
which
was
better
than
zinc–thiazole
(ZT:
=
7.3
μg/mL)
thiodiazole–copper
(TC:
65.5
μg/mL);
A25
Phomopsis
sp.
(Ps),
17.2
azoxystrobin
(Az:
22.3
μg/mL).
In
vivo
inhibition
tests
performed
kiwifruit
for
rice
leaves
A12.
At
200
curative
activity
leaf
blight
40.7%,
that
ZT
(37.2%)
TC
(32.9%),
protective
44.8%,
(39.5%)
(34.6%).
kiwi
soft
rot
disease
70.1%,
Az
(62.8%).
Preliminary
elucidation
possible
mechanisms
action
carried
out
by
experiments
fluorescence
microscopy,
scanning
electron
formation
biofilms,
density
functional
theory
calculations,
so
on.
Pest Management Science,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 12, 2024
A
large
number
of
pathogenic
fungi
have
caused
serious
damage
to
the
global
crop
yield,
and
drug
resistance
is
always
a
topic
that
cannot
be
avoided
for
traditional
fungicides.
Therefore,
finding
efficient,
green,
low-toxic
fungicides
our
primary
task,
which
brings
opportunities
development
natural
product
green
pesticides.
Journal of Heterocyclic Chemistry,
Journal Year:
2022,
Volume and Issue:
60(2), P. 241 - 251
Published: Sept. 9, 2022
Abstract
Pyrimidine
is
an
important
heterocyclic
ring
with
various
activities,
which
are
widely
used
in
the
field
of
pesticides
and
medicines.
In
this
paper,
a
series
1,2,4‐triazolo[1,5‐
]pyrimidine‐7‐amine
compounds
(
V1
–
V16
)
containing
1,2,4‐oxadiazole
moiety
were
designed
synthesized.
Their
structures
confirmed
by
1
H
NMR,
13
C
19
F
HRMS.
The
biological
activity
results
showed
that
V5
,
V6
V7
V9
V10
V12
V13
possessed
good
against
Mythimna
separate
at
500
ppm,
while
compound
V4
exhibited
moderate
Aphis
medicagini
ppm.
Furthermore,
V3
displayed
fungicidal
Pseudoperonospora
cubensis
200
