Table 3.
ADME and toxicity properties prediction of the two potent derivatives 15a and 15b.
| Properties | 15a | 15b | ||
|---|---|---|---|---|
| Absorption | ||||
| P-glycoprotein substrate | Yes | Yes | ||
| P-glycoprotein I inhibitor | Yes | Yes | ||
| P-glycoprotein II inhibitor | Yes | Yes | ||
| Distribution | ||||
| BBB permeability (log BB) | −0.766 | −0.766 | ||
| CNS permeability (log PS) | −2.439 | −2.413 | ||
| Metabolism | ||||
| CYP1A2 inhibitior | Yes | Yes | ||
| CYP2C19 inhibitior | Yes | Yes | ||
| CYP2C9 inhibitior | Yes | Yes | ||
| CYP2D6 inhibitior | No | No | ||
| CYP3A4 inhibitior | Yes | Yes | ||
| Toxicity | ||||
| Ames test (Mutagenicity) | Mutagen | Mutagen | ||
| Carcinogenicity (Mouse) | Positive | Positive | ||
| Carcinogenicity (Rat) | Negative | Positive | ||
| hERG inhibition | High risk | High risk | ||
= Inhibitior, Non-Mutagen, Negative carcinogenicity, and Low risk.
= Non-inhibitior, Mutagen, Positive carcinogenicity, and High risk.