Table 1.
SAR of phenyl ring of 1 for CpIMPDH inhibition.
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---|---|---|---|
ID | R1 | IC50 (nM)
|
|
(−) BSA | (+) BSA | ||
1 | 2,4-di-ClPh | 44 ± 8 | 120 ± 10 |
41 | 2-ClPh | 19 ± 2 | 50 ± 10 |
42 | 4-ClPh | 105 ± 17 | 118 ± 3 |
43 | Ph | 40 ± 5 | 50 ± 20 |
44 | 4-OMePh | 28 ± 2 | 34 ± 5 |
45 | 3-ClPh | 20 ± 7 | 32 ± 8 |
46 | 2,3-di-ClPh | 3 ± 1 | 11 ± 1 |
47 | 2,6-di-ClPh | >5000* | n.d |
48 | 1-naphthyl | 9 ± 3 | 14 ± 6 |
49 | 1-(4-Cl-naphthyl) | 27 ± 1 | 53 ± 9 |
One determination, n.d. = not determined.