|
Антибактериальная in vitro и in vivo активность
Препарат
Антибактериальная
активность in vitro
Антибактериальная активность
in vivo
МПК, мкг/мл
Количество
живо
тных
в
группе
,
голов
Доза
, мг
/кг
Средняя продолжительность
жизни, сут
Синегнойная
палочка
№
509
Кишечн
ая
па
ло
чк
а
№
1749
Полевой
шт
амм
кишечно
й
палочки
Музейный
шт
ам
м
золоти
стого
стафилококк
а (
№
209
Р
)
Музейный
шт
ам
м
кишечной
палочки
(
№
1749)
Музейный
шт
ам
м
синегн
ойной
палочки
(
№
509)
Макроцикл (4)
3,13
1,56
1,56
10
10
6.5 5.5 5.0
10
15
7.5 6.0 6.5
10
20
8.0 6.5 7.0
Эритромицин 3,13
1,56
3,13
10
15
7.5 6.0 6.5
Кларитромицин
3,13
0,78
1,56
10
15
8.0 7.5 7.0
Спирамицин 1,56
0,09
0,09
10
12
8.7 8.0 7.0
Фуразолидон 3,13
6,25
3,13
10
3
6.0 5.5 3.2
Тетрациклин 3,13
3,13
3,13
10
10
7.5 7.2 7.2
Контроль
- - - 10
-
1.7 2.0 1.7
1. Г. Ю. Ишмуратов, М. П. Яковлева, Г. Р. Мингалеева и др., Химия природ. соедин.,
395, 2009.
2. Г. Ю. Ишмуратов, Г. Р. Мингалеева, М. П. Яковлева и др., Химия природ. соедин.,
400, 2009.
3. Г. Ю. Ишмуратов, М. П. Яковлева, Г. Р. Мингалеева и др., Бутлеровские сообщения,
14, 59, 2008.
4. В. Н. Одиноков, Г. Ю. Ишмуратов, Л. П. Боцман и др., Химия природ. соедин., 423,
1992.
РАЗДЕЛ III
СТЕНДОВЫЕ ДОКЛАДЫ
86
SYNTHESIS OF NEW (+)-3-CARENE DERIVATIVES
AND EVALUATION OF THEIR CATALYTIC EFFICIENCY FOR
EPOXIDE RING OPENING REACTION
L. Bets, Z.
Ribkovskaia,
L. Vlad,
M. Freund, A. Zamfir,
S. Wei, S.B. Tsogoeva,
F.Z. Macaev
Institute of Chemistry, Academy of Sciences of Moldova, Academiei 3,
MD-2028, Chisinau, Moldova
University of Erlangen-Nuremberg, Henkestrasse 42, 91054 Erlangen, Germany
flmacaev@cc.acad.md and flmacaev@gmail.com
Asymmetric synthesis mediated by organocatalysts becomes more and more important for the devel-
opment of industrial processes as well as scientific research [1]. Cooperative catalysis with chiral thiourea-
based bifunctional molecules has recently been recognized as a new and exciting strategy in asymmetric or-
ganocatalysis [2, 3]. On the other hand, monoterpenes derived amine readily accessible, could be easily con-
verted to chiral thioureas and thioxopyrimidinones as well.
In this communication we report the results of the epoxide ring opening reaction of the model
6 with aniline in the presence of the chiral thioureas 2-3, prepared from monoterpene (+)-
3 carene 1.
N
H
N
H
S
O
R
N N
O
S
2 ( meta) R=OMe
3 ( meta) R=NH
2
4 ( para) R=OMe
5 ( para) R=NH
2
1
*
O
H
2
N
+
Cat.(10 mol%)
solvents
RT, 2 days
N
H
OH
*
6
7
8
All the above-mentioned compounds act as catalysts for epoxide ring opening reaction. The data on the
influence of the catalyst structure on the enantioselectivity [4] of the reaction will be discussed.
The authors gratefully acknowledge generous financial support from the BMBF (DLR) -ASM
(project 09.820.05.08.GF) and World Federation of Scientists.
1. Berkessel, H. Gröger, Asymmetric Organocatalysis: From Biomimetic Concepts to Applications in
Asymmetric Synthesis, Wiley-VCH, Weinheim, 2004.
2. S. J. Connon, Chem. Eur. J., 12, 5418, 2006.
3. G. Doyle, E. N. Jacobsen, Chem. Rev., 107, 5713, 2007.
4. Enantioselectivities were determined by chiral HPLC analysis (Daicel Chiralpak IA) in comparison
with authentic racemic material.
87
SYNTHESIS AND STRUCTURE OF COPPER(II) COMPLEX
WITH ECONALOZE
G. Dulcevscaia, T. Yudin, V. Sargorovschi, E. Stingaci, V.Ch. Kravtsov,
S.G. Baca, S. Pogrebnoi, F. Macaev
Institute of Chemistry, Academy of Sciences of Moldova, Academiei 3,
MD-2028, Chisinau, Moldova;
Institute of Applied Physics, Academy of Sciences of Moldova, Academiei 5,
MD-2028 Chisinau, Moldova
flmacaev@cc.acad.md and flmacaev@gmail.com
Our previous report has revealed that econazole nitrate exhibited in vitro anti-tubercular activi-
ty against Mycobacterium tuberculosis H
37
Rv (ATCC 27294) [1]. In order to investigate the essen-
tial structural features for the anti-mycobacterial activity of such type compound, the synthesis and
X-ray studies of new copper(II) carboxylates with econazole (L), a mononuclear complex
[Cu(L)
2
(O
2
CMe)
2
]·2H
2
O and coordination polymer [Cu(L)
2
(Pht)]
∞
(where H
2
Pht – o-phthalic acid)
were initiated [2].
In continue this work a new copper(II) complex [Cu(L)
2
Cl
2
] ( 1) with econazole has been syn-
thesized and characterized by X-ray crystallography, IR spectroscopy and thermogravimetric anal-
ysis. Compound 1 crystallizes in triclinic space group P (No. 2), a = 8.657(2) Å, b = 9.062(2) Å, c
= 13.797(3) Å, α = 107.698(2)°, β = 107.840(3)°, γ = 92.215(3)°. X-ray crystallographic study of 1
reveled the centrosymmetrical mononuclear [Cu(L)
2
Cl
2
] complex in which Cu(II) atom coordinates
in trans-positions two econazole molecules and
two chlorine atoms resulted in square-planar sur-
rounding of the metal (Fig.). The econazole mo-
lecules act as neutral monodentate ligands and
coordinate to copper by the nitrogen atom of im-
idazole group. The distances Cu(1)–N(1) =
2.006(1) Å and Cu(1)–Cl(5)= 2.2564 (5) Å, the
angle N(1)
−Cu(1)−Cl(5) = 89.90(4)°. The imida-
zole group is nearly coplanar with the coordina-
tion plane of copper atom and forms dihedral angle of 18.31°. The bond distances C–N and C–C of
imidazole group are in the range of 1.331 - 1.383 Å and indicate their delocalization. Intermolecu-
lar aromatic
π-π interactions as well as C−H···Cl and Cl···Cl interactions stabilize the crystal struc-
ture of 1.
This study is supported by Supreme Council for Science and Technological Development of
Moldova, project 09.836.05.02A. The authors acknowledge the assistance of Dr. Yu. Wang in the
collection of crystallographic data sets for 1.
1. V. Munteanu (Sargorovschi). VI All-Russian Scientific Seminar with young scientific school “Che-
mistry and medicine”. Ufa, Russia. P. 220, 2007.
2. V. Sargorovschi, G. Dulcevscaia, E. Stingachi, S. Pogrebnoi, V. Kravtsov, Yu. Simonov, Ya.
Lipkowski, S.G. Baca, F. Macaev. The proceeding of the International Conference dedicated to the 50
th
an-
niversary from the foundation of the Institute of Chemistry of the Academy of Sciences of Moldova. 26-28
May 2009, Chisinau, Moldova. PP-043. P. 101.
88
Do'stlaringiz bilan baham: |
