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. 2018 May 24;33(1):972–977. doi: 10.1080/14756366.2018.1474211

Table 1.

hIMPDH2 enzyme inhibition of MPA amides (14–28 at 10 µM).

Compound R hIMPDH2 enzyme
% Inhibitiona IC50 (µM)±SDb
1 Mycophenolic acid 99.90 ± 1.20 0.25 ± 0.03
14 (S)-(−)-α-Methylbenzyl 59.15 ± 1.91 n.d.c
15 (R)-(+)-α-Methylbenzyl 73.94 ± 2.84 0.82 ± 0.32
16 2-Chlorobenzyl 72.04 ± 1.11 0.73 ± 0.06
17 2-Furfuryl 67.18 ± 4.16 n.d.c
18 4-Methoxybenzyl 96.13 ± 2.51 0.33 ± 0.11
19 4-Methylbenzyl 73.42 ± 3.62 0.60 ± 0.13
20 4-Chlorobenzyl 81.36 ± 1.95 0.57 ± 0.11
21 4-Pyridylmethyl 57.38 ± 1.02 n.d.c
22 2-Pyridylmethyl 59.38 ± 1.81 n.d.c
23 2-Methylbenzyl 84.00 ± 2.13 0.50 ± 0.18
24 4-Phenylbutyl 93.62 ± 3.17 0.48 ± 0.02
25 3,4-(Methylenedioxy)benzyl 87.09 ± 4.54 0.51 ± 0.08
26 2-Morpholinoethyl 36.05 ± 3.86 n.d.c
27 3-Methoxyphenyl 30.82 ± 2.82 n.d.c
28 4-Methoxyphenyl 54.84 ± 1.15 n.d.c

aAll the data are expressed as ± SD (results are average of duplicate analysis).

bAll the data are expressed as ± SD (results are average of triplicate analysis). IC50 value was determined when the inhibitory rate of compound is higher than 70% at the concentration of 10 µM.

cn.d.: not determined.