char = A;code = 65 char = n;code = 110 char = t;code = 116 char = i;code = 105 char = p;code = 112 char = r;code = 114 char = o;code = 111 char = t;code = 116 char = o;code = 111 char = z;code = 122 char = o;code = 111 char = a;code = 97 char = l;code = 108 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = 1;code = 49 char = -;code = 45 char = p;code = 112 char = h;code = 104 char = e;code = 101 char = n;code = 110 char = e;code = 101 char = t;code = 116 char = h;code = 104 char = y;code = 121 char = l;code = 108 char = -;code = 45 char = 4;code = 52 char = -;code = 45 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = n;code = 110 char = o;code = 111 char = p;code = 112 char = i;code = 105 char = p;code = 112 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = d;code = 100 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = v;code = 118 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.char = A;code = 65 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = 4;code = 52 char = 4;code = 52 char = ;code = 32 char = 4;code = 52 char = -;code = 45 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = n;code = 110 char = o;code = 111 char = p;code = 112 char = i;code = 105 char = p;code = 112 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = d;code = 100 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = v;code = 118 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 = 32 char = w;code = 119 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = s;code = 115 char = c;code = 99 char = r;code = 114 char = e;code = 101 char = e;code = 101 char = n;code = 110 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = ;code = 32 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = r;code = 114 char = o;code = 111 char = ;code = 32 char = a;code = 97 char = g;code = 103 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = f;code = 102 char = o;code = 111 char = u;code = 117 char = r;code = 114 char = ;code = 32 char = p;code = 112 char = r;code = 114 char = o;code = 111 char = t;code = 116 char = o;code = 111 char = z;code = 122 char = o;code = 111 char = a;code = 97 char = n;code = 110 char = ;code = 32 char = p;code = 112 char = a;code = 97 char = r;code = 114 char = a;code = 97 char = s;code = 115 char = i;code = 105 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = (;code = 40 char = T;code = 84 char = r;code = 114 char = y;code = 121 char = p;code = 112 char = a;code = 97 char = n;code = 110 char = o;code = 111 char = s;code = 115 char = o;code = 111 char = m;code = 109 char = a;code = 97 char = ;code = 32 char = b;code = 98 char = r;code = 114 char = u;code = 117 char = c;code = 99 char = e;code = 101 char = i;code = 105 char = ;code = 32 char = r;code = 114 char = h;code = 104 char = o;code = 111 char = d;code = 100 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = e;code = 101 char = n;code = 110 char = s;code = 115 char = e;code = 101 char = ,;code = 44 char = ;code = 32 char = T;code = 84 char = r;code = 114 char = y;code = 121 char = p;code = 112 char = a;code = 97 char = n;code = 110 char = o;code = 111 char = s;code = 115 char = o;code = 111 char = m;code = 109 char = a;code = 97 char = ;code = 32 char = c;code = 99 char = r;code = 114 char = u;code = 117 char = z;code = 122 char = i;code = 105 char = ,;code = 44 char = ;code = 32 char = L;code = 76 char = e;code = 101 char = i;code = 105 char = s;code = 115 char = h;code = 104 char = m;code = 109 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = a;code = 97 char = ;code = 32 char = d;code = 100 char = o;code = 111 char = n;code = 110 char = o;code = 111 char = v;code = 118 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = ,;code = 44 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = P;code = 80 char = l;code = 108 char = a;code = 97 char = s;code = 115 char = m;code = 109 char = o;code = 111 char = d;code = 100 char = i;code = 105 char = u;code = 117 char = m;code = 109 char = ;code = 32 char = f;code = 102 char = a;code = 97 char = l;code = 108 char = c;code = 99 char = i;code = 105 char = p;code = 112 char = a;code = 97 char = r;code = 114 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 char = e;code = 101 char = e;code = 101 char = n;code = 110 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = i;code = 105 char = f;code = 102 char = i;code = 105 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = 2;code = 50 char = 9;code = 57 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = u;code = 117 char = l;code = 108 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = e;code = 101 char = l;code = 108 char = y;code = 121 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = g;code = 103 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = b;code = 98 char = l;code = 108 char = o;code = 111 char = o;code = 111 char = d;code = 100 char = s;code = 115 char = t;code = 116 char = r;code = 114 char = e;code = 101 char = a;code = 97 char = m;code = 109 char = -;code = 45 char = f;code = 102 char = o;code = 111 char = r;code = 114 char = m;code = 109 char = ;code = 32 char = T;code = 84 char = .;code = 46 char = ;code = 32 char = b;code = 98 char = .;code = 46 char = ;code = 32 char = r;code = 114 char = h;code = 104 char = o;code = 111 char = d;code = 100 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = e;code = 101 char = n;code = 110 char = s;code = 115 char = e;code = 101 char = ;code = 32 char = t;code = 116 char = r;code = 114 char = y;code = 121 char = p;code = 112 char = o;code = 111 char = m;code = 109 char = a;code = 97 char = s;code = 115 char = t;code = 116 char = i;code = 105 char = g;code = 103 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = ,;code = 44 char = ;code = 32 char = w;code = 119 char = i;code = 105 char = t;code = 116 char = h;code = 104 char = ;code = 32 char = 5;code = 53 char = 0;code = 48 char = %;code = 37 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = h;code = 104 char = i;code = 105 char = b;code = 98 char = i;code = 105 char = t;code = 116 char = o;code = 111 char = r;code = 114 char = y;code = 121 char = ;code = 32 char = c;code = 99 char = o;code = 111 char = n;code = 110 char = c;code = 99 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = r;code = 114 char = a;code = 97 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 char = s;code = 115 char = ;code = 32 char = (;code = 40 char = I;code = 73 char = C;code = 67 char = 5;code = 53 char = 0;code = 48 char = );code = 41 char = ;code = 32 char = r;code = 114 char = a;code = 97 char = n;code = 110 char = g;code = 103 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = f;code = 102 char = r;code = 114 char = o;code = 111 char = m;code = 109 char = ;code = 32 char = 0;code = 48 char = .;code = 46 char = 1;code = 49 char = 2;code = 50 char = ;code = 32 char = t;code = 116 char = o;code = 111 char = ;code = 32 char = 1;code = 49 char = 0;code = 48 char = ;code = 32 char = m;code = 109 char = i;code = 105 char = c;code = 99 char = r;code = 114 char = o;code = 111 char = M;code = 77 char = ,;code = 44 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = 3;code = 51 char = 3;code = 51 char = ;code = 32 char = c;code = 99 char = o;code = 111 char = m;code = 109 char = p;code = 112 char = o;code = 111 char = u;code = 117 char = n;code = 110 char = d;code = 100 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = g;code = 103 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = c;code = 99 char = h;code = 104 char = l;code = 108 char = o;code = 111 char = r;code = 114 char = o;code = 111 char = q;code = 113 char = u;code = 117 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = -;code = 45 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = p;code = 112 char = y;code = 121 char = r;code = 114 char = i;code = 105 char = m;code = 109 char = e;code = 101 char = t;code = 116 char = h;code = 104 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = -;code = 45 char = r;code = 114 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = s;code = 115 char = t;code = 116 char = a;code = 97 char = n;code = 110 char = t;code = 116 char = ;code = 32 char = K;code = 75 char = 1;code = 49 char = ;code = 32 char = s;code = 115 char = t;code = 116 char = r;code = 114 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = P;code = 80 char = .;code = 46 char = ;code = 32 char = f;code = 102 char = a;code = 97 char = l;code = 108 char = c;code = 99 char = i;code = 105 char = p;code = 112 char = a;code = 97 char = r;code = 114 char = u;code = 117 char = m;code = 109 char = ;code = 32 char = (;code = 40 char = I;code = 73 char = C;code = 67 char = 5;code = 53 char = 0;code = 48 char = ;code = 32 char = r;code = 114 char = a;code = 97 char = n;code = 110 char = g;code = 103 char = e;code = 101 char = ,;code = 44 char = ;code = 32 char = 0;code = 48 char = .;code = 46 char = 1;code = 49 char = 7;code = 55 char = ;code = 32 char = t;code = 116 char = o;code = 111 char = ;code = 32 char = 5;code = 53 char = ;code = 32 char = m;code = 109 char = i;code = 105 char = c;code = 99 char = r;code = 114 char = o;code = 111 char = M;code = 77 char = );code = 41 char = .;code = 46 char = ;code = 32 char = I;code = 73 char = n;code = 110 char = ;code = 32 char = a;code = 97 char = d;code = 100 char = d;code = 100 char = i;code = 105 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 char = ,;code = 44 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = v;code = 118 char = e;code = 101 char = n;code = 110 char = ;code = 32 char = c;code = 99 char = o;code = 111 char = m;code = 109 char = p;code = 112 char = o;code = 111 char = u;code = 117 char = n;code = 110 char = d;code = 100 char = s;code = 115 char = ;code = 32 char = d;code = 100 char = i;code = 105 char = s;code = 115 char = p;code = 112 char = l;code = 108 char = a;code = 97 char = y;code = 121 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = a;code = 97 char = g;code = 103 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = t;code = 116 char = r;code = 114 char = a;code = 97 char = c;code = 99 char = e;code = 101 char = l;code = 108 char = l;code = 108 char = u;code = 117 char = l;code = 108 char = a;code = 97 char = r;code = 114 char = ;code = 32 char = T;code = 84 char = .;code = 46 char = ;code = 32 char = c;code = 99 char = r;code = 114 char = u;code = 117 char = z;code = 122 char = i;code = 105 char = ;code = 32 char = a;code = 97 char = m;code = 109 char = a;code = 97 char = s;code = 115 char = t;code = 116 char = i;code = 105 char = g;code = 103 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = s;code = 115 char = a;code = 97 char = m;code = 109 char = e;code = 101 char = ;code = 32 char = r;code = 114 char = a;code = 97 char = n;code = 110 char = g;code = 103 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = r;code = 114 char = e;code = 101 char = f;code = 102 char = e;code = 101 char = r;code = 114 char = e;code = 101 char = n;code = 110 char = c;code = 99 char = e;code = 101 char = ;code = 32 char = d;code = 100 char = r;code = 114 char = u;code = 117 char = g;code = 103 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = n;code = 110 char = i;code = 105 char = d;code = 100 char = a;code = 97 char = z;code = 122 char = o;code = 111 char = l;code = 108 char = e;code = 101 char = ;code = 32 char = (;code = 40 char = I;code = 73 char = C;code = 67 char = 5;code = 53 char = 0;code = 48 char = ,;code = 44 char = ;code = 32 char = 1;code = 49 char = .;code = 46 char = 9;code = 57 char = 7;code = 55 char = ;code = 32 char = m;code = 109 char = i;code = 105 char = c;code = 99 char = r;code = 114 char = o;code = 111 char = M;code = 77 char = );code = 41 char = ;code = 32 char = b;code = 98 char = u;code = 117 char = t;code = 116 char = ;code = 32 char = w;code = 119 char = e;code = 101 char = r;code = 114 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = l;code = 108 char = s;code = 115 char = o;code = 111 char = ;code = 32 char = c;code = 99 char = y;code = 121 char = t;code = 116 char = o;code = 111 char = t;code = 116 char = o;code = 111 char = x;code = 120 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = t;code = 116 char = o;code = 111 char = ;code = 32 char = L;code = 76 char = -;code = 45 char = 6;code = 54 char = ;code = 32 char = c;code = 99 char = e;code = 101 char = l;code = 108 char = l;code = 108 char = s;code = 115 char = ,;code = 44 char = ;code = 32 char = s;code = 115 char = h;code = 104 char = o;code = 111 char = w;code = 119 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = l;code = 108 char = i;code = 105 char = t;code = 116 char = t;code = 116 char = l;code = 108 char = e;code = 101 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = f;code = 102 char = o;code = 111 char = r;code = 114 char = ;code = 32 char = T;code = 84 char = .;code = 46 char = ;code = 32 char = c;code = 99 char = r;code = 114 char = u;code = 117 char = z;code = 122 char = i;code = 105 char = .;code = 46 char = ;code = 32 char = N;code = 78 char = o;code = 111 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = u;code = 117 char = l;code = 108 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = t;code = 116 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = s;code = 115 char = h;code = 104 char = o;code = 111 char = w;code = 119 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = t;code = 116 char = e;code = 101 char = r;code = 114 char = e;code = 101 char = s;code = 115 char = t;code = 116 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = t;code = 116 char = i;code = 105 char = l;code = 108 char = e;code = 101 char = i;code = 105 char = s;code = 115 char = h;code = 104 char = m;code = 109 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = a;code = 97 char = l;code = 108 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = a;code = 97 char = g;code = 103 char = a;code = 97 char = i;code = 105 char = n;code = 110 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = a;code = 97 char = x;code = 120 char = e;code = 101 char = n;code = 110 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = a;code = 97 char = m;code = 109 char = a;code = 97 char = s;code = 115 char = t;code = 116 char = i;code = 105 char = g;code = 103 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = L;code = 76 char = .;code = 46 char = ;code = 32 char = d;code = 100 char = o;code = 111 char = n;code = 110 char = o;code = 111 char = v;code = 118 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = .;code = 46 char = ;code = 32 char = T;code = 84 char = o;code = 111 char = ;code = 32 char = o;code = 111 char = u;code = 117 char = r;code = 114 char = ;code = 32 char = k;code = 107 char = n;code = 110 char = o;code = 111 char = w;code = 119 char = l;code = 108 char = e;code = 101 char = d;code = 100 char = g;code = 103 char = e;code = 101 char = ,;code = 44 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = i;code = 105 char = s;code = 115 char = ;code = 32 char = i;code = 105 char = s;code = 115 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = f;code = 102 char = i;code = 105 char = r;code = 114 char = s;code = 115 char = t;code = 116 char = ;code = 32 char = r;code = 114 char = e;code = 101 char = p;code = 112 char = o;code = 111 char = r;code = 114 char = t;code = 116 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = t;code = 116 char = i;code = 105 char = t;code = 116 char = r;code = 114 char = y;code = 121 char = p;code = 112 char = a;code = 97 char = n;code = 110 char = o;code = 111 char = s;code = 115 char = o;code = 111 char = m;code = 109 char = a;code = 97 char = l;code = 108 char = ;code = 32 char = a;code = 97 char = c;code = 99 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = i;code = 105 char = t;code = 116 char = y;code = 121 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = l;code = 108 char = e;code = 101 char = c;code = 99 char = u;code = 117 char = l;code = 108 char = e;code = 101 char = s;code = 115 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = a;code = 97 char = r;code = 114 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = 4;code = 52 char = -;code = 45 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = n;code = 110 char = o;code = 111 char = p;code = 112 char = i;code = 105 char = p;code = 112 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = s;code = 115 char = k;code = 107 char = e;code = 101 char = l;code = 108 char = e;code = 101 char = t;code = 116 char = o;code = 111 char = n;code = 110 char = .;code = 46 char = <;code = 60 char = b;code = 98 char = r;code = 114 char = /;code = 47 char = >;code = 62 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.
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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