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. 2023 May 24;257:115487. doi: 10.1016/j.ejmech.2023.115487

Table 4.

SAR exploration of substituent groups at C-2 and N-3 positions of quinazolin-4-onea.

Compd R4 R5 IC50 (μM)
D1 Image 39 Image 40 0.477 ± 0.078
D2 Image 41 Image 42 1.005 ± 0.136
D3 Image 43 Image 44 0.290 ± 0.030
D4 Image 45 Image 46 0.386 ± 0.017
D5 Image 47 Image 48 0.692 ± 0.119
D6 Image 49 Image 50 0.107 ± 0.023
D7 Image 51 Image 52 0.239 ± 0.028
D8 Image 53 Image 54 0.100 ± 0.012
D9 Image 55 Image 56 0.284 ± 0.028
D10 Image 57 Image 58 0.131 ± 0.022
D11 Image 59 Image 60 0.502 ± 0.038
D12 Image 61 Image 62 0.466 ± 0.040
C7 Image 63 Image 64 0.085 ± 0.006

2.3.

a

C7 was used as the positive control. Inhibitory activity against SARS-CoV-2 Mprowas determined with the FRET protease activity assay. Values represent a mean ± SD of at least three independent experiments.