Table 4.
Benzamide SAR: Physicochemical, In Vitro ADME, Antimalarial, and Cytotoxicity Data
| ||||||
|---|---|---|---|---|---|---|
| Compd | LogD7.4 | PSA (Å2) | Kinetic Sol6.5 (μg/mL) | h/m CLint(μL/min/mg protein) | P. falciparumIC50 (μM) | L6 IC50 (μM) |
| 30 | 0.9 | 59.1 | >100 | 19/18 | 9.4 | 160 |
| 31 | 0.9 | 59.1 | >100 | 11/10 | 11 | 190 |
| 32 | 2.1 | 46.2 | 50-100 | 11/110 | 0.13 | 96 |
| 33 | 2.0 | 70.0 | 25–50 | <7/160 | 0.39 | 150 |
| 34 | 1.1 | 66.4 | 25–50 | 61/84a | 15 | 84 |
| 35 | 1.3 | 66.4 | >100 | 16/60 | 5.1 | 210 |
| 36 | 2.1 | 46.2 | >100 | 13/43 | 1.3 | 110 |
| 37 | 1.2 | 66.4 | 12.5–25 | 7/36 | 1.1 | 200 |
Apparent non-NADPH-mediated degradation.