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. Author manuscript; available in PMC: 2014 May 23.
Published in final edited form as: J Med Chem. 2013 May 13;56(10):4028–4043. doi: 10.1021/jm400241j

Table 2.

SAR of amide α-position of 1 for CpIMPDH inhibition.

graphic file with name nihms479334u2.jpg
ID X R1 IC50 (nM)
(−) BSA (+) BSA
50 CH2 2,4-di-ClPh >5000* n.d
51 CMe2 4-ClPh >5000* n.d
52 CH-i-Pr 1-naphthyl 24 ± 2 57 ± 5
53 (R)-CHMe 1-naphthyl 400 ± 70 380 ± 60
54 (S)-CHMe 1-naphthyl 6.1 ± 0.5 8 ± 3
55 (S)-CHMe 2,3-di-ClPh 1.2 ± 0.2 3.5 ± 0.7
56 (S)-CHMe 2-Cl,3-CF3Ph 9 ± 1 52 ± 5
57 (S)-CHMe 2-Cl,3-NO2Ph 2.3 ± 0.9 6 ± 4
58 (S)-CHMe 2,3-di-OMePh 50 ± 10 60 ± 20
*

One determination, n.d. = not determined.