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. 2014 Dec 4;57(24):10544–10550. doi: 10.1021/jm501527z

Table 3. Modifications of the Acetamide and 4-Oxo-[1]benzopyrano[4,3-c]pyrazole Regions of 8k for CpIMPDH Inhibition.

graphic file with name jm-2014-01527z_0006.jpg

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