char = D;code = 68 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = g;code = 103 char = n;code = 110 char = ,;code = 44 char = ;code = 32 char = s;code = 115 char = y;code = 121 char = n;code = 110 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = s;code = 115 char = i;code = 105 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = n;code = 110 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 = 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 = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = i;code = 105 char = m;code = 109 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 = 45 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = h;code = 104 char = y;code = 121 char = b;code = 98 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = s;code = 115 char = .;code = 46 result sql = Design, synthesis and in vitro antiprotozoal activity of benzimidazole-pentamidine hybrids.
Design, synthesis and in vitro antiprotozoal activity of benzimidazole-pentamidine hybrids.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 = t;code = 116 char = e;code = 101 char = n;code = 110 char = ;code = 32 char = n;code = 110 char = o;code = 111 char = v;code = 118 char = e;code = 101 char = l;code = 108 char = ;code = 32 char = h;code = 104 char = y;code = 121 char = b;code = 98 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = s;code = 115 char = ;code = 32 char = f;code = 102 char = r;code = 114 char = o;code = 111 char = m;code = 109 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = i;code = 105 char = m;code = 109 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 = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = w;code = 119 char = e;code = 101 char = r;code = 114 char = e;code = 101 char = ;code = 32 char = p;code = 112 char = r;code = 114 char = e;code = 101 char = p;code = 112 char = a;code = 97 char = r;code = 114 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = u;code = 117 char = s;code = 115 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = a;code = 97 char = ;code = 32 char = s;code = 115 char = h;code = 104 char = o;code = 111 char = r;code = 114 char = t;code = 116 char = ;code = 32 char = s;code = 115 char = y;code = 121 char = n;code = 110 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = t;code = 116 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = r;code = 114 char = o;code = 111 char = u;code = 117 char = t;code = 116 char = e;code = 101 char = .;code = 46 char = ;code = 32 char = E;code = 69 char = a;code = 97 char = c;code = 99 char = h;code = 104 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 = ;code = 32 char = w;code = 119 char = a;code = 97 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 = 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 = t;code = 116 char = h;code = 104 char = e;code = 101 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 = ;code = 32 char = T;code = 84 char = r;code = 114 char = i;code = 105 char = c;code = 99 char = h;code = 104 char = o;code = 111 char = m;code = 109 char = o;code = 111 char = n;code = 110 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = v;code = 118 char = a;code = 97 char = g;code = 103 char = i;code = 105 char = n;code = 110 char = a;code = 97 char = l;code = 108 char = i;code = 105 char = s;code = 115 char = ,;code = 44 char = ;code = 32 char = G;code = 71 char = i;code = 105 char = a;code = 97 char = r;code = 114 char = d;code = 100 char = i;code = 105 char = a;code = 97 char = ;code = 32 char = l;code = 108 char = a;code = 97 char = m;code = 109 char = b;code = 98 char = l;code = 108 char = i;code = 105 char = a;code = 97 char = ,;code = 44 char = ;code = 32 char = E;code = 69 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = o;code = 111 char = e;code = 101 char = b;code = 98 char = a;code = 97 char = ;code = 32 char = h;code = 104 char = i;code = 105 char = s;code = 115 char = t;code = 116 char = o;code = 111 char = l;code = 108 char = y;code = 121 char = t;code = 116 char = i;code = 105 char = c;code = 99 char = a;code = 97 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 = m;code = 109 char = e;code = 101 char = x;code = 120 char = i;code = 105 char = c;code = 99 char = a;code = 97 char = n;code = 110 char = a;code = 97 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 = b;code = 98 char = e;code = 101 char = r;code = 114 char = g;code = 103 char = h;code = 104 char = e;code = 101 char = i;code = 105 char = ,;code = 44 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = ;code = 32 char = c;code = 99 char = o;code = 111 char = m;code = 109 char = p;code = 112 char = a;code = 97 char = r;code = 114 char = i;code = 105 char = s;code = 115 char = o;code = 111 char = n;code = 110 char = ;code = 32 char = w;code = 119 char = i;code = 105 char = t;code = 116 char = h;code = 104 char = ;code = 32 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = m;code = 109 char = e;code = 101 char = t;code = 116 char = r;code = 114 char = o;code = 111 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 = 46 char = ;code = 32 char = S;code = 83 char = o;code = 111 char = m;code = 109 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = a;code = 97 char = l;code = 108 char = o;code = 111 char = g;code = 103 char = u;code = 117 char = e;code = 101 char = s;code = 115 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 = h;code = 104 char = i;code = 105 char = g;code = 103 char = h;code = 104 char = ;code = 32 char = b;code = 98 char = i;code = 105 char = o;code = 111 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 = 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 = l;code = 108 char = o;code = 111 char = w;code = 119 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 = 109 char = o;code = 111 char = l;code = 108 char = a;code = 97 char = r;code = 114 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 = (;code = 40 char = I;code = 73 char = C;code = 67 char = (;code = 40 char = 5;code = 53 char = 0;code = 48 char = );code = 41 char = <;code = 60 char = 1;code = 49 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 = 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 = f;code = 102 char = i;code = 105 char = r;code = 114 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 = ,;code = 44 char = ;code = 32 char = w;code = 119 char = h;code = 104 char = i;code = 105 char = c;code = 99 char = h;code = 104 char = ;code = 32 char = m;code = 109 char = a;code = 97 char = k;code = 107 char = e;code = 101 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = m;code = 109 char = ;code = 32 char = s;code = 115 char = i;code = 105 char = g;code = 103 char = n;code = 110 char = i;code = 105 char = f;code = 102 char = i;code = 105 char = c;code = 99 char = a;code = 97 char = n;code = 110 char = t;code = 116 char = l;code = 108 char = y;code = 121 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = r;code = 114 char = e;code = 101 char = ;code = 32 char = p;code = 112 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = a;code = 97 char = n;code = 110 char = ;code = 32 char = e;code = 101 char = i;code = 105 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = r;code = 114 char = ;code = 32 char = s;code = 115 char = t;code = 116 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = a;code = 97 char = r;code = 114 char = d;code = 100 char = .;code = 46 char = ;code = 32 char = 1;code = 49 char = ,;code = 44 char = 5;code = 53 char = -;code = 45 char = b;code = 98 char = i;code = 105 char = s;code = 115 char = [;code = 91 char = 4;code = 52 char = -;code = 45 char = (;code = 40 char = 5;code = 53 char = -;code = 45 char = m;code = 109 char = e;code = 101 char = t;code = 116 char = h;code = 104 char = o;code = 111 char = x;code = 120 char = y;code = 121 char = -;code = 45 char = 1;code = 49 char = H;code = 72 char = -;code = 45 char = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = i;code = 105 char = m;code = 109 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 = 45 char = 2;code = 50 char = -;code = 45 char = y;code = 121 char = l;code = 108 char = );code = 41 char = p;code = 112 char = h;code = 104 char = e;code = 101 char = n;code = 110 char = o;code = 111 char = x;code = 120 char = y;code = 121 char = ];code = 93 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = n;code = 110 char = e;code = 101 char = ;code = 32 char = (;code = 40 char = 2;code = 50 char = );code = 41 char = ;code = 32 char = w;code = 119 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = 3;code = 51 char = -;code = 45 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = 9;code = 57 char = -;code = 45 char = f;code = 102 char = o;code = 111 char = l;code = 108 char = d;code = 100 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = r;code = 114 char = e;code = 101 char = ;code = 32 char = p;code = 112 char = o;code = 111 char = t;code = 116 char = e;code = 101 char = n;code = 110 char = t;code = 116 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 = G;code = 71 char = .;code = 46 char = ;code = 32 char = l;code = 108 char = a;code = 97 char = m;code = 109 char = b;code = 98 char = l;code = 108 char = i;code = 105 char = a;code = 97 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = a;code = 97 char = n;code = 110 char = ;code = 32 char = m;code = 109 char = e;code = 101 char = t;code = 116 char = r;code = 114 char = o;code = 111 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 = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 char = e;code = 101 char = ,;code = 44 char = ;code = 32 char = r;code = 114 char = e;code = 101 char = s;code = 115 char = p;code = 112 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 = 46 char = ;code = 32 char = T;code = 84 char = h;code = 104 char = i;code = 105 char = s;code = 115 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 = ;code = 32 char = w;code = 119 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = 2;code = 50 char = 3;code = 51 char = -;code = 45 char = ,;code = 44 char = ;code = 32 char = 1;code = 49 char = 0;code = 48 char = 8;code = 56 char = -;code = 45 char = ,;code = 44 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = 1;code = 49 char = 3;code = 51 char = -;code = 45 char = f;code = 102 char = o;code = 111 char = l;code = 108 char = d;code = 100 char = ;code = 32 char = m;code = 109 char = o;code = 111 char = r;code = 114 char = e;code = 101 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 = t;code = 116 char = h;code = 104 char = a;code = 97 char = n;code = 110 char = ;code = 32 char = p;code = 112 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = a;code = 97 char = m;code = 109 char = i;code = 105 char = d;code = 100 char = i;code = 105 char = n;code = 110 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 = 84 char = .;code = 46 char = ;code = 32 char = v;code = 118 char = a;code = 97 char = g;code = 103 char = i;code = 105 char = n;code = 110 char = a;code = 97 char = l;code = 108 char = i;code = 105 char = s;code = 115 char = ,;code = 44 char = ;code = 32 char = E;code = 69 char = .;code = 46 char = ;code = 32 char = h;code = 104 char = i;code = 105 char = s;code = 115 char = t;code = 116 char = o;code = 111 char = l;code = 108 char = y;code = 121 char = t;code = 116 char = i;code = 105 char = c;code = 99 char = a;code = 97 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = L;code = 76 char = .;code = 46 char = ;code = 32 char = m;code = 109 char = e;code = 101 char = x;code = 120 char = i;code = 105 char = c;code = 99 char = a;code = 97 char = n;code = 110 char = a;code = 97 char = ,;code = 44 char = ;code = 32 char = r;code = 114 char = e;code = 101 char = s;code = 115 char = p;code = 112 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 = 46 char = ;code = 32 char = S;code = 83 char = t;code = 116 char = u;code = 117 char = d;code = 100 char = y;code = 121 char = i;code = 105 char = n;code = 110 char = g;code = 103 char = ;code = 32 char = f;code = 102 char = u;code = 117 char = r;code = 114 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = r;code = 114 char = ;code = 32 char = s;code = 115 char = t;code = 116 char = r;code = 114 char = u;code = 117 char = c;code = 99 char = t;code = 116 char = u;code = 117 char = r;code = 114 char = e;code = 101 char = -;code = 45 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 = r;code = 114 char = e;code = 101 char = l;code = 108 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 = h;code = 104 char = i;code = 105 char = p;code = 112 char = s;code = 115 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = r;code = 114 char = o;code = 111 char = u;code = 117 char = g;code = 103 char = h;code = 104 char = ;code = 32 char = t;code = 116 char = h;code = 104 char = e;code = 101 char = ;code = 32 char = u;code = 117 char = s;code = 115 char = e;code = 101 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = b;code = 98 char = i;code = 105 char = o;code = 111 char = i;code = 105 char = s;code = 115 char = o;code = 111 char = s;code = 115 char = t;code = 116 char = e;code = 101 char = r;code = 114 char = i;code = 105 char = c;code = 99 char = ;code = 32 char = s;code = 115 char = u;code = 117 char = b;code = 98 char = s;code = 115 char = t;code = 116 char = i;code = 105 char = t;code = 116 char = u;code = 117 char = t;code = 116 char = i;code = 105 char = o;code = 111 char = n;code = 110 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 = s;code = 115 char = e;code = 101 char = ;code = 32 char = h;code = 104 char = y;code = 121 char = b;code = 98 char = r;code = 114 char = i;code = 105 char = d;code = 100 char = s;code = 115 char = ;code = 32 char = s;code = 115 char = h;code = 104 char = o;code = 111 char = u;code = 117 char = l;code = 108 char = d;code = 100 char = ;code = 32 char = p;code = 112 char = r;code = 114 char = o;code = 111 char = v;code = 118 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = ;code = 32 char = n;code = 110 char = e;code = 101 char = w;code = 119 char = ;code = 32 char = l;code = 108 char = e;code = 101 char = a;code = 97 char = d;code = 100 char = s;code = 115 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 = 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 = d;code = 100 char = i;code = 105 char = s;code = 115 char = e;code = 101 char = a;code = 97 char = s;code = 115 char = e;code = 101 char = s;code = 115 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 ten novel hybrids from benzimidazole and pentamidine were prepared using a short synthetic route. Each compound was tested in vitro against the protozoa Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica, Leishmania mexicana, and Plasmodium berghei, in comparison with pentamidine and metronidazole. Some analogues showed high bioactivity in the low micromolar range (IC(50)<1 microM) against the first four protozoa, which make them significantly more potent than either standard. 1,5-bis[4-(5-methoxy-1H-benzimidazole-2-yl)phenoxy]pentane (2) was 3- and 9-fold more potent againstG. lamblia than metronidazole and pentamidine, respectively. This compound was 23-, 108-, and 13-fold more active than pentamidine against T. vaginalis, E. histolytica and L. mexicana, respectively. Studying further structure-activity relationships through the use of bioisosteric substitution in these hybrids should provide new leads against protozoal diseases.
Publication: Bioorg. Med. Chem. Lett. 2008 Jun 1 ;18(11)::3147-51. :doi: 10.1016/j.bmcl.2008.05.009.
Publication Date: 2008 Jun 1
Study Author(s): Torres-Gómez, Héctor;Hernández-Núñez, Emanuel;León-Rivera, Ismael;Guerrero-Alvarez, Jorge;Cedillo-Rivera, Roberto;Moo-Puc, Rosa;Argotte-Ramos, Rocío;Rodríguez-Gutiérrez, María Del Carmen;Chan-Bacab, Manuel Jesús;Navarrete-Vázquez, Gabriel;
Institution: Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico.
Shortcut link to this study:
A series of ten novel hybrids from benzimidazole and pentamidine were prepared using a short synthetic route. Each compound was tested in vitro against the protozoa Trichomonas vaginalis, Giardia lamblia, Entamoeba histolytica, Leishmania mexicana, and Plasmodium berghei, in comparison with pentamidine and metronidazole. Some analogues showed high bioactivity in the low micromolar range (IC(50)<1 microM) against the first four protozoa, which make them significantly more potent than either standard. 1,5-bis[4-(5-methoxy-1H-benzimidazole-2-yl)phenoxy]pentane (2) was 3- and 9-fold more potent againstG. lamblia than metronidazole and pentamidine, respectively. This compound was 23-, 108-, and 13-fold more active than pentamidine against T. vaginalis, E. histolytica and L. mexicana, respectively. Studying further structure-activity relationships through the use of bioisosteric substitution in these hybrids should provide new leads against protozoal diseases.
PMID: 18486471