Table 3.
Phenotypic activity of dihydropyrazolone bio‐isosteres against intracellular amastigotes of T. cruzi (Tulahuen strain) and MRC‐5 cells.
|
| ||||
|---|---|---|---|---|
|
Cmpd |
Headgroup |
pIC50 [a] |
SI[b] |
|
|
|
|
T. cruzi |
MRC‐5 |
|
|
95 |
|
4.5 |
4.3 |
2 |
|
98 |
|
<4.2 |
<4.2 |
‐ |
|
99 |
|
6.3 |
4.8 |
32 |
|
104 |
|
5.0 |
4.6 |
3 |
|
109 |
|
4.8 |
<4.2 |
>4 |
[a] All reported values are within a standard deviation of ±0.2 and the result of at least n=2. [b] The selectivity index is calculated by dividing the cytotoxicity (IC50) by the T. cruzi activity (IC50).