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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5732_Библиотеки_им_академика_М_И_Перельмана
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Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 251
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[32]
320.3
8
(2E,2'E)-N,N'-ethane-1,2-diylbis(3-phenylprop-
2-enamide)
1.63 5.10
a
198.00 618.00
e
121
[34]
575.7
0
N-[9-[2-(benzyloxy)phenyl]-3,3,6,6-tetramethyl-
1,8-dioxo-2,3,4,5,6,7,8,9-octahydro-10(1H)-
acridinyl]
Isonicotinamide
<0.10
<0.17
d
>62.17
>108.00
e
>635
[33]
492.5
2
3-[3-Benzo[b]furan-2-yl-5-(2-hydroxyphenyl)-
4,5-dihydro-
1H-1-pyrazolylcarbonyl]-1-ethyl-7-methyl-1,4-
dihydro[1,8]
naphthyridin-4-one
1.20
g
2.44 >77.82
>158.00
e
>64
Данная книга находится в списке для перевода на русский язык сайта https://meduniver.com/
252 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[36]
645.9
2
(4S)-4-benzyl-1-((25)-1-(2-(((S)-5-benzyl-2-
iminoimidazolidin-1-yl)methyl)pyrrolidin-1-yl)-
3-phenylpropan-2-yl)-3-
(cicloheptylmethyl)imidazolidin-2-imino
3.90 6.04 39.48 61.12 10
[48]
577.6
0
1-cyclopropyl-7-(8-(4-methoxybenzyl)-
3,4,5,6,7,8-hexahydroisoquinolim-2-(1H)-yl-1,4-
dihydro-6-fluoro-8-methoxy-5-nitro-4-
oxoquinoline-3-carboxylic acid
0.09 0.16
d
62.38 108.00
e
675
[49]
532.0
0
Quinolone derivative 0.05 0.09
d
>77.67
>146.00
e
>155
3
NHN
NH
N
N
N
NH
Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 253
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[28]
492.4
8
7-(4-((benzo[
d][1,3]dioxol-5-yl)methyl)piperazin-1-yl)-1-
cyclopropyl-1,4-dihydro-6-nitro-4-oxoquinoline-
3-carboxylic acid
0.04 0.08
d
62.54 127.00
e
1563
[37]
431.5
1
Naphthalen-2-yl-9-naphthalen-2-ylmethylene-
6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-2-
ylamine
3.12
d
7.23 31.12
g
72.12 10
[38] 410.4
4-(cyclopropylcarbonyl)-N-[(4,6-
dimethoxypyrimidin-2-yl)carbamoyl]-1-methyl-
1H-pyrazole-5-sulfonamide
3.13-
6.31
g
7.63-
15.37
≥300.00
g
≥731.00
≥96
or
≥48
N
N
NH
2
Данная книга находится в списке для перевода на русский язык сайта https://meduniver.com/
254 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[35]
356.2
2
2-(pyridin-4-ylcarbonyl)-N-[2-
(trifluoromethoxy)phenyl]hydrazinecarbothioam
ide
0.21 0.58
d
>208.00
e
>583.90 >990
[27]
490.4
8
1-cyclopropyl-7-(3,5-dimethyl-4-(3-
nitropropanoyl)
piperazin-1-yl)-6-fluoro-8-methoxy-4-oxo-1,4-
dihydroquinoline-3-carboxylic acid
0.08 0.16
d
62.29 127.00
e
779
[39]
326.3
4
(2E)-3-(5-nitrofuran -2-yl)-1-[4-(piperidin-1-
yl)phenyl]prop-2-en-1-one
0.06 0.19
a
113.89 349.00
e
1837
[40]
419.4
5
ethyl 4-[3-(4-fluorophenyl)-1-phenyl-
1H-pyrazol-4-yl]-6-methyl-2-oxo-1,2,3,4-
tetrahydropyrimidine-5 carboxylate
0.02
b
0.05 >10.00
e
>23.84 >500
256 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[51]
502.5
3
4’-[5-(4-fluorophermyl)pyridin-3-yl]-1-methyl-
dispiro-[indan-2,2- pyrrolidine-3,2-indan]-1,3,1-
´trione
0.06 0.12
d
>62.50
e
>124.37
>103
6
[43]
262.3
0
1,1-dimethylaminobenzofuro-[2,3-b]-quinoline <0.20
b
<0.76 >30.00
e
>114.37 >150
(a) REMA; (b) MABA; (c) BACTEC; (d) Agar dilution method (NCCLS); (e) MTT; (f) Neutral Red; (g) Other.
Данная книга находится в списке для перевода на русский язык сайта https://meduniver.com/
Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 257
Table 2: Class compounds of different synthetic organic compounds and the activity against MTB H37Rv, cytotoxicity to cells others
than VERO and the calculation of selectivity index of their best compound
Refs.
Class Compounds
MW
Best Compound
MIC IC
50
SI
μg/mL μM μg/mL μM
IC
50
/
MIC
J774 Macrophage cell line from mouse
[30]
479.45 glycosyl thioacetamide derivative 1.56
d
3.25 >15.60
g
>32.54 >10
[52]
222.31 2-acetylpyridine N4(ethyl)
thiosemicarbazone
3.13ª 14.80ª 625.00ª 2811.00ª 190
[53]
380.37 4-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-N-
(pyrimidin-2-yl)benzenesulfonamide
3.90
a
10.25 312.50
a
821.57 80
[37]
431.51 Naphthalen-2-yl-9-naphthalen-2-ylmethylene-
6,7,8,9-tetrahydro-5H-cycloheptapyrimidin-2-
ylamine
3.12
d
7.23 31.12
g
72.12 10
N
CH
3
N
NH NH
S
CH
3
N
N
NH
2
258 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
Refs.
Class Compounds
MW
Best Compound
MIC IC
50
SI
μg/mL μM μg/mL μM
IC
50
/
MIC
HepG2 hepato cell line from human liver carcinoma
[54]
346.51 1-({1-[3-(4-hydroxyphenyl)-1-
methylpropyl]piperidin-4-yl}methyl)piperidin-4-ol
2.70 7.80
d
56.13 162.00
g
20
[45]
482.45 1-Cyclopropyl-6-fluoro-4-oxo-7-{4-[4-
(fluorobenzoyl)hydrazonomethyl]
piperazin-1-yl}-1,4-dihydroquinoline-3-carboxylic
acid
1.00
g
2.07 >617.54 >1280.00
e
>618
PBMC peripheral blood mononuclear cells from human
[55]
320.42 6-Isopentyl-1,2,3,4-tetrahydrobenzo[a]phenazin-
5(7H)-one
<3.12 9.75 >25.00 >78.20 >8
N
OH
N
CH
3
OH
Данная книга находится в списке для перевода на русский язык сайта https://meduniver.com/
Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 255
Refs.
Class Compounds
MW Best Compound
MIC IC
50
SI
μg/m
L
μM μg/mL μM
IC
50
/
MIC
[41]
506.0
0
Diethyl 1-(2-chloro-phenyl)-1,4-dihydro-2,6-
dimethyl-4-(1,3-diphenyl-1h-pyrazol-4-yl)
pyridine-3,5-dicarboxylote
0.02
b
0.04 >10.00
e
>19.76 >500
[50]
566.6
2
3-Benzyl-2-[4-fluoro-2-(1-imidazol-1-yl-ethyl)-
phenoxy]-6-(4-phenyl-[1,2,3]triazol-1-yl)-
quinoline
3.13
c
5.52
>100.00
g
>176.48 32
[42]
295.2
6
7-methyl-3-(4’-fluoro)phenylquinoxaline-2-
carbonitrile
1,4-di-N-oxide
<0.20
b
<0.68 100.00
e
338.68 >500
Tuberculosis
Organic Compounds to Combat Neglected Tropical Diseases 259
Refs.
Class Compounds
MW
Best Compound
MIC IC
50
SI
μg/mL μM μg/mL μM
IC
50
/
MIC
[45]
482.45 1-Cyclopropyl-6-fluoro-4-oxo-7-{4-[4-
(fluorobenzoyl)hydrazonomethyl]
piperazin-1-yl}-1,4-dihydroquinoline-3-carboxylic
acid
1.00
g
2.07 368.11 763.00
e
368
HEK 293T cells from human embryonic kidney
[46]
308.37 N,N'-bis[(2S)-1-hydroxybutan-2-yl]benzene-1,2-
dicarboxamid
0.20 0.65
g
75.24 244.00
e
375
[56]
284.20 5-nitro-N-(5-
nitrothiazol-2-yl)furan-2-carboxamide
1.56 5.48
d
28.42 100.00
f
18
A549 cells from human adenocarcinomic alveolar basal epitelial cells
N
S
NO
2
NH
O
O
O
2
N
Данная книга находится в списке для перевода на русский язык сайта https://meduniver.com/
260 Organic Compounds to Combat Neglected Tropical Diseases Santos et al.
Refs.
Class Compounds
MW
Best Compound
MIC IC
50
SI
μg/mL μM μg/mL μM
IC
50
/
MIC
[57]
241.33 4-amino-5-(4-isopropyl-1,3-thiazol-2-yl)-4H-1,2,4-
triazole-3-thiol
8.00
d
33.15 60.33 250.00
e
7
THP-1 cells from acute monocytic leukemia
[58]
418.25 2-Chloro-N-(4-chloro-3-(N-(4-methoxypyrimidin-2-
ylcarbamoyl)
sulfamoyl)phenyl)acetamide
10.00
d
23.91 179.70
e
429.65 18
NIH 3T3 from mouse embryonic fibroblast
[59]
490.43 2-[2-(4-bromophenyl)-4-phenyl-3-
quinolyl]sulfanyl-5-methyl-1,3,4-thiadiazole
1.57 3.20
d
1005.38 2050.00
e
640
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