char = S;code = 83 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 = 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 = o;code = 111 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 = o;code = 111 char = f;code = 102 char = ;code = 32 char = N;code = 78 char = i;code = 105 char = t;code = 116 char = a;code = 97 char = z;code = 122 char = o;code = 111 char = x;code = 120 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = T;code = 84 char = i;code = 105 char = z;code = 122 char = o;code = 111 char = x;code = 120 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = :;code = 58 char = ;code = 32 char = a;code = 97 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 = a;code = 97 char = t;code = 116 char = i;code = 105 char = v;code = 118 char = e;code = 101 char = ;code = 32 char = s;code = 115 char = t;code = 116 char = u;code = 117 char = d;code = 100 char = y;code = 121 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 = i;code = 105 char = r;code = 114 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 = b;code = 98 char = r;code = 114 char = o;code = 111 char = a;code = 97 char = d;code = 100 char = -;code = 45 char = s;code = 115 char = p;code = 112 char = e;code = 101 char = c;code = 99 char = t;code = 116 char = r;code = 114 char = u;code = 117 char = m;code = 109 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 = 46 result sql = Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.char = W;code = 87 char = e;code = 101 char = ;code = 32 char = h;code = 104 char = a;code = 97 char = v;code = 118 char = e;code = 101 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 = z;code = 122 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = t;code = 116 char = w;code = 119 char = o;code = 111 char = ;code = 32 char = n;code = 110 char = e;code = 101 char = w;code = 119 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = o;code = 111 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 = o;code = 111 char = f;code = 102 char = ;code = 32 char = N;code = 78 char = i;code = 105 char = t;code = 116 char = a;code = 97 char = z;code = 122 char = o;code = 111 char = x;code = 120 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = ;code = 32 char = (;code = 40 char = N;code = 78 char = I;code = 73 char = T;code = 84 char = );code = 41 char = ;code = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = T;code = 84 char = i;code = 105 char = z;code = 122 char = o;code = 111 char = x;code = 120 char = a;code = 97 char = n;code = 110 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = ;code = 32 char = (;code = 40 char = T;code = 84 char = I;code = 73 char = Z;code = 90 char = );code = 41 char = ,;code = 44 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 = B;code = 66 char = o;code = 111 char = t;code = 116 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 = s;code = 115 char = ;code = 32 char = w;code = 119 char = e;code = 101 char = r;code = 114 char = e;code = 101 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 = s;code = 115 char = i;code = 105 char = x;code = 120 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 = (;code = 40 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 = i;code = 105 char = n;code = 110 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = t;code = 116 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 = 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 = 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 = 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 = 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 = 32 char = a;code = 97 char = n;code = 110 char = d;code = 100 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 = 41 char = .;code = 46 char = ;code = 32 char = C;code = 67 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 = 1;code = 49 char = ;code = 32 char = (;code = 40 char = b;code = 98 char = e;code = 101 char = n;code = 110 char = z;code = 122 char = o;code = 111 char = l;code = 108 char = o;code = 111 char = g;code = 103 char = u;code = 117 char = e;code = 101 char = ;code = 32 char = o;code = 111 char = f;code = 102 char = ;code = 32 char = N;code = 78 char = I;code = 73 char = T;code = 84 char = );code = 41 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 = b;code = 98 char = r;code = 114 char = o;code = 111 char = a;code = 97 char = d;code = 100 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 = e;code = 101 char = f;code = 102 char = f;code = 102 char = e;code = 101 char = c;code = 99 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 = ;code = 32 char = a;code = 97 char = l;code = 108 char = l;code = 108 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 = 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 = 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 = I;code = 73 char = C;code = 67 char = (;code = 40 char = 5;code = 53 char = 0;code = 48 char = );code = 41 char = ';code = 39 char = s;code = 115 char = <;code = 60 char = 5;code = 53 char = ;code = 32 char = &;code = 38 char = #;code = 35 char = 9;code = 57 char = 5;code = 53 char = 6;code = 54 char = ;;code = 59 char = M;code = 77 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 = f;code = 102 char = i;code = 105 char = v;code = 118 char = e;code = 101 char = -;code = 45 char = t;code = 116 char = i;code = 105 char = m;code = 109 char = e;code = 101 char = s;code = 115 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 = N;code = 78 char = I;code = 73 char = T;code = 84 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 = 8;code = 56 char = -;code = 45 char = t;code = 116 char = i;code = 105 char = m;code = 109 char = e;code = 101 char = s;code = 115 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 = 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 = 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 = G;code = 71 char = .;code = 46 char = ;code = 32 char = i;code = 105 char = n;code = 110 char = t;code = 116 char = e;code = 101 char = s;code = 115 char = t;code = 116 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 = 46 char = ;code = 32 char = I;code = 73 char = t;code = 116 char = ;code = 32 char = w;code = 119 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = 1;code = 49 char = 0;code = 48 char = -;code = 45 char = t;code = 116 char = i;code = 105 char = m;code = 109 char = e;code = 101 char = s;code = 115 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 = 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 = a;code = 97 char = n;code = 110 char = d;code = 100 char = ;code = 32 char = i;code = 105 char = t;code = 116 char = ;code = 32 char = w;code = 119 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = s;code = 115 char = e;code = 101 char = v;code = 118 char = e;code = 101 char = n;code = 110 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 = t;code = 116 char = h;code = 104 char = a;code = 97 char = n;code = 110 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 = v;code = 118 char = e;code = 101 char = r;code = 114 char = s;code = 115 char = u;code = 117 char = s;code = 115 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 = 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 = c;code = 99 char = o;code = 111 char = u;code = 117 char = l;code = 108 char = d;code = 100 char = ;code = 32 char = b;code = 98 char = e;code = 101 char = ;code = 32 char = c;code = 99 char = o;code = 111 char = n;code = 110 char = s;code = 115 char = i;code = 105 char = d;code = 100 char = e;code = 101 char = r;code = 114 char = e;code = 101 char = d;code = 100 char = ;code = 32 char = a;code = 97 char = s;code = 115 char = ;code = 32 char = a;code = 97 char = ;code = 32 char = n;code = 110 char = e;code = 101 char = w;code = 119 char = ;code = 32 char = b;code = 98 char = r;code = 114 char = o;code = 111 char = a;code = 97 char = d;code = 100 char = ;code = 32 char = s;code = 115 char = p;code = 112 char = e;code = 101 char = c;code = 99 char = t;code = 116 char = r;code = 114 char = u;code = 117 char = m;code = 109 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 = g;code = 103 char = e;code = 101 char = n;code = 110 char = t;code = 116 char = .;code = 46 char = <;code = 60 char = b;code = 98 char = r;code = 114 char = /;code = 47 char = >;code = 62 result sql = We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Plasmodium berghei, Leishmania mexicana and Trypanosoma cruzi). Compound 1 (benzologue of NIT) showed broad antiprotozoal effect against all parasites tested, showing IC(50)'s<5 μM. This compound was five-times more active than NIT, and 18-times more potent than metronidazole against G. intestinalis. It was 10-times more active than pentamidine against L. mexicana, and it was sevenfold more potent than benznidazole versus T. cruzi. This compound could be considered as a new broad spectrum antiprotozoal agent.
Publication: Bioorg. Med. Chem. Lett. 2011 May 15 ;21(10)::3168-71. :doi: 10.1016/j.bmcl.2011.02.100.
Publication Date: 2011 May 15
Study Author(s): Navarrete-Vazquez, Gabriel;Chávez-Silva, Fabiola;Argotte-Ramos, Rocío;Rodríguez-Gutiérrez, María del Carmen;Chan-Bacab, Manuel Jesús;Cedillo-Rivera, Roberto;Moo-Puc, Rosa;Hernández-Nuñez, Emanuel;
Institution: Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico.
[email protected]
Shortcut link to this study:
We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Plasmodium berghei, Leishmania mexicana and Trypanosoma cruzi). Compound 1 (benzologue of NIT) showed broad antiprotozoal effect against all parasites tested, showing IC(50)'s<5 μM. This compound was five-times more active than NIT, and 18-times more potent than metronidazole against G. intestinalis. It was 10-times more active than pentamidine against L. mexicana, and it was sevenfold more potent than benznidazole versus T. cruzi. This compound could be considered as a new broad spectrum antiprotozoal agent.
PMID: 21397502