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. Author manuscript; available in PMC: 2018 Oct 15.
Published in final edited form as: Bioorg Med Chem. 2017 Jul 13;25(20):5194–5202. doi: 10.1016/j.bmc.2017.07.020

Table 2.

Inhibition of the hydrolysis of model substrates by β-galactosidases from bovine liver (5 mM HEPES buffer, pH 7.50) and A. oryzae (50 mM acetate buffer, pH 5.00) in the presence of galactonoamidines 1d, 1u–y; R = -CH2-C6H4-CH3

Compound Glycon structure β-galactosidase (Bovine Liver) β-galactosidase (A. oryzae)
Ki ± ΔKi [nM] IC50 [nM] Ki ± ΔKi [nM] IC50 [nM]
Galactonoamidines with modifications in the glycon
1d graphic file with name nihms903308t21.jpg 0.07 ± 0.01 57.6 8.0 ± 0.5 36
1u graphic file with name nihms903308t22.jpg 0.60 ± 0.07 850 2,400 ± 300 33,300
1v graphic file with name nihms903308t23.jpg 1,500 ± 220 10,800 3,400 ± 300 41,400
1w graphic file with name nihms903308t24.jpg 840 ± 60 9,200 1,400 ± 200 40,700
Control compounds
1x graphic file with name nihms903308t25.jpg 2,000 ± 200 > 50,000 150 ± 20 830
1y graphic file with name nihms903308t26.jpg 2,700 ± 260 8,700 615 ± 30 > 50,000