Table 2. Stereochemical Investigation around the Original Hit.
T. b. brucei EC50 (μM)a | MRC-5 EC50 (μM)a | mouse microsomal intrinsic clearance (mL min–1 g–1) | |
---|---|---|---|
1 | 0.027 | >50 | 4.4 |
(S)-26 | 41 | >50 | 4.0 |
(R)-27 | 0.029 | >50 | 3.6 |
EC50 values are shown as mean values of two or more determinations. Standard deviation is typically within 2–3-fold from the EC50.