Table 3. Modifications of the Acetamide and 4-Oxo-[1]benzopyrano[4,3-c]pyrazole Regions of 8k for CpIMPDH Inhibition.
ID | method | R1 | R2 | R3 | X | Y | IC50(nM) |
---|---|---|---|---|---|---|---|
8k | A | H | H | H | O | C=O | 20 ± 4 |
8l | C | Me | H | H | O | C=O | >5000 |
8m | C | H | Me | H | O | C=O | 63 ± 11 |
8n | C | H | H | Me | O | C=O | 2000 |
13e | D | H | H | H | O | CH2 | 70 ± 27 |
13f | D | H | H | H | CH2 | CH2 | 100 ± 30 |