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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 3.

SAR of the pyridine ring of 1 for CpIMPDH inhibition.

graphic file with name nihms479334u3.jpg
ID X R1 R2 IC50 (nM)
(−) BSA (+) BSA
59 Me 2,4-di-ClPh Ph >5000* n.d
60 Me 2,4-di-ClPh 3-Py 150 ± 20 600 ± 200
61 Me 2,4-di-ClPh 2-Py 210 ± 20 800 ± 200
62 (S)-Me 2,3-di-ClPh graphic file with name nihms479334t1.jpg 1.4 ± 0.3 2.3 ± 0.4
63 (S)-Me 1-naphthyl graphic file with name nihms479334t2.jpg 2.7 ± 0.7 4.0 ± 0.9
64 Me 1-(4-Cl-naphthyl) graphic file with name nihms479334t3.jpg 28 ± 6 70 ± 10
65 (S)-Me 2,3-di-ClPh graphic file with name nihms479334t4.jpg 17 ± 6 30 ± 10
66 (S)-Me 1-naphthyl graphic file with name nihms479334t5.jpg 26 ± 5 50 ± 5
67 Me 1-naphthyl graphic file with name nihms479334t6.jpg >5000* n.d
*

One determination, n.d. = not determined.