Table 1. SAR of 2-Position Substituted 7-Azaindole Inhibitors.
cmpd | R | X | bDNA EC90a (μM) |
---|---|---|---|
6 | H | H | 0.001 |
12 | CH2OH | H | 0.028 |
15 | CH2OH | (R)-F | 0.01 |
16 | CH3 | H | 0.28 |
17 | cyclopropyl | H | >3.3 |
19 | COOH | H | 2.2 |
20 | C=NOH | H | 0.091 |
21a | CH(OH)CH3(R/S) | H | 0.027 |
21b | CH(OH)CH3(R/S) | H | 0.46 |
The concentration of test compound resulting in viral RNA levels equal to that of 10% of the control wells was reported as EC90.