Table 4.
Compound No. |
Structure | Aq. Solubility (µg/mL) |
Metabolic Stability (t1/2) | |||||
---|---|---|---|---|---|---|---|---|
pH | Mouse | Human | ||||||
7.4 | 5.0 | 3.0 | liver S9 | plasma | liver micro somes |
plasm a |
||
1a | 63 | 75 | 74 | 15 min | - | 4.7 h | - | |
8g | 30 | 51 | 75 | 11 min | 2.4 h | 5.3 h | >24 h | |
8p | 18 | 18 | <15 | 20 min | - | 42 min | - | |
8n | 4 minb | 3.6 h | ||||||
8a | 58 | 25 | 20 | |||||
8j | 28 | 43 | 48 |
Detailed solubility and metabolism procedures in Experimental Section
Tested against mouse liver microsomes