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. Author manuscript; available in PMC: 2011 May 13.
Published in final edited form as: J Med Chem. 2010 May 13;53(9):3594–3601. doi: 10.1021/jm901857d

Table 4. DART-carboxamides.

graphic file with name nihms194521u4.jpg
Compound R4 R5 IC50 TD50 TI Log TI
1524 H Et 6.8 259 38 1.6
16 Et Et 11 23 2.1 0.3
17 H Me 15 ≥320 37 1.6
18 H Bn 0.67 ≥320 839 2.9
19 H 4-MeThiazole 0.65 ≥320 865 2.9
20 H p-FBn 0.47 72 153 2.2
21 H p-CH3Bn 0.51 169 331 2.5
22 H p-CF3Bn 0.34 ≥320 1654 3.2
23 H 3,4-F2Bn 0.47 78 166 2.2
24 H 3,5-F2Bn 0.36 ≥320 1562 3.2
25 H 3,5-Br2Bn 0.81 ≥320 694 2.8
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