Table 6.
SAR around hit series 2 b.
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---|---|---|---|---|
Compd | R2 | R1 | R | TbTryS IC50 [μm] |
43 | H | H | H | >50 |
44 | H | 2-CH3 | H | 15 |
45 | H | 2-Cl | H | 25 |
46 | H | H | 2,5-di-Cl | 16 |
47 | H | H | 4-NHCOCH3 | 5.9 |
48 | H | H | 4-OCH3 | 11 |
49 | H | 2-CH3 | 4-OCH3 | 4.0 |
50 | H | 2-CH3 | 4-NHCOCH3 | 1.7 |
51 | H | 2-Cl | 4-NHCOCH3 | 3.7 |
52 | CH3 | H | 4-NHCOCH3 | >50 |