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char = n;code = 110
char = t;code = 116
char = i;code = 105
char = p;code = 112
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char = o;code = 111
char = t;code = 116
char = o;code = 111
char = z;code = 122
char = o;code = 111
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char = l;code = 108
char = ;code = 32
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char = v;code = 118
char = i;code = 105
char = t;code = 116
char = y;code = 121
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char = o;code = 111
char = f;code = 102
char = ;code = 32
char = 1;code = 49
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char = p;code = 112
char = h;code = 104
char = e;code = 101
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char = e;code = 101
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char = h;code = 104
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char = 4;code = 52
char = -;code = 45
char = a;code = 97
char = m;code = 109
char = i;code = 105
char = n;code = 110
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char = i;code = 105
char = p;code = 112
char = e;code = 101
char = r;code = 114
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char = d;code = 100
char = i;code = 105
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char = d;code = 100
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char = a;code = 97
char = t;code = 116
char = i;code = 105
char = v;code = 118
char = e;code = 101
char = s;code = 115
char = .;code = 46
result sql = Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.
Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.
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char = f;code = 102
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char = 4;code = 52
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char = 4;code = 52
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char = p;code = 112
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char = e;code = 101
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char = ;code = 32
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char = T;code = 84
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char = p;code = 112
char = a;code = 97
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char = s;code = 115
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char = m;code = 109
char = a;code = 97
char = ;code = 32
char = c;code = 99
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char = u;code = 117
char = z;code = 122
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char = ,;code = 44
char = ;code = 32
char = L;code = 76
char = e;code = 101
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char = s;code = 115
char = h;code = 104
char = m;code = 109
char = a;code = 97
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char = i;code = 105
char = a;code = 97
char = ;code = 32
char = d;code = 100
char = o;code = 111
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char = o;code = 111
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char = i;code = 105
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char = d;code = 100
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char = P;code = 80
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char = a;code = 97
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char = u;code = 117
char = m;code = 109
char = );code = 41
char = .;code = 46
char = ;code = 32
char = T;code = 84
char = h;code = 104
char = i;code = 105
char = s;code = 115
char = ;code = 32
char = s;code = 115
char = c;code = 99
char = r;code = 114
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char = e;code = 101
char = n;code = 110
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char = n;code = 110
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char = i;code = 105
char = d;code = 100
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char = i;code = 105
char = f;code = 102
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char = d;code = 100
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char = m;code = 109
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char = a;code = 97
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char = b;code = 98
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char = d;code = 100
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char = a;code = 97
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char = -;code = 45
char = f;code = 102
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char = m;code = 109
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char = T;code = 84
char = .;code = 46
char = ;code = 32
char = b;code = 98
char = .;code = 46
char = ;code = 32
char = r;code = 114
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char = d;code = 100
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char = e;code = 101
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char = p;code = 112
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char = ,;code = 44
char = ;code = 32
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char = t;code = 116
char = h;code = 104
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char = 5;code = 53
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char = %;code = 37
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char = h;code = 104
char = i;code = 105
char = b;code = 98
char = i;code = 105
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char = y;code = 121
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char = r;code = 114
char = a;code = 97
char = t;code = 116
char = i;code = 105
char = o;code = 111
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char = s;code = 115
char = ;code = 32
char = (;code = 40
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char = C;code = 67
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char = ,;code = 44
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char = 3;code = 51
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char = o;code = 111
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char = n;code = 110
char = d;code = 100
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char = a;code = 97
char = c;code = 99
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char = i;code = 105
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char = a;code = 97
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char = K;code = 75
char = 1;code = 49
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char = T;code = 84
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result sql = A series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum). This screening identified 29 molecules selectively active against bloodstream-form T. b. rhodesiense trypomastigotes, with 50% inhibitory concentrations (IC50) ranging from 0.12 to 10 microM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 microM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 microM) but were also cytotoxic to L-6 cells, showing little selectivity for T. cruzi. None of the molecules tested showed interesting antileishmanial activity against axenic amastigotes of L. donovani. To our knowledge, this is the first report of the antitrypanosomal activity of molecules bearing the 4-aminopiperidine skeleton.

Publication: Antimicrob. Agents Chemother. 2009 Sep ;53(9)::3815-21. :doi: 10.1128/AAC.00124-09.
Publication Date: 2009 Sep
Study Author(s): Dardonville, Christophe;Fernández-Fernández, Cristina;Gibbons, Sarah-Louise;Jagerovic, Nadine;Nieto, Lidia;Ryan, Gary;Kaiser, Marcel;Brun, Reto;
Institution: Instituto de Química Médica, CSIC, Juan de la Cierva 3, E-28006 Madrid, Spain. [email protected]
Shortcut link to this study:
A series of 44 4-aminopiperidine derivatives was screened in vitro against four protozoan parasites (Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani, and Plasmodium falciparum). This screening identified 29 molecules selectively active against bloodstream-form T. b. rhodesiense trypomastigotes, with 50% inhibitory concentrations (IC50) ranging from 0.12 to 10 microM, and 33 compounds active against the chloroquine- and pyrimethamine-resistant K1 strain of P. falciparum (IC50 range, 0.17 to 5 microM). In addition, seven compounds displayed activity against intracellular T. cruzi amastigotes in the same range as the reference drug benznidazole (IC50, 1.97 microM) but were also cytotoxic to L-6 cells, showing little selectivity for T. cruzi. None of the molecules tested showed interesting antileishmanial activity against axenic amastigotes of L. donovani. To our knowledge, this is the first report of the antitrypanosomal activity of molecules bearing the 4-aminopiperidine skeleton.
PMID: 19564359

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