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. 2019 Oct 9;29(23):126727. doi: 10.1016/j.bmcl.2019.126727

Table 1.

MERS-CoV inhibitory activity of 3-acyl-2-amino-1,4-dihydroquinolin-4(1H)-one derivatives.

graphic file with name fx1_lrg.jpg

Cpd X Y Z W R1 R2 IC50 (μM)a CC50 (μM)b SIc
1 H Cl H CF3 Me i-PrNH- 0.77 >25 33
6a H H H i-Pr Me i-PrNH- >25 – –
6b H Me H Me Me i-PrNH- >25 – –
6c H Cl H CF3 Ph i-PrNH- >25 – –
6d H Cl H CF3 Me 2,4-F2-PhNH- 0.15 7.3 78
6e H Cl H F Me 2,4-F2-PhNH- 0.98 >25 26
6f H Cl H NO2 Me 2,4-F2-PhNH- 1.16 >25 21
6g H F H F Me 2,4-F2-PhNH- 1.06 >25 25
6h Cl Cl H Cl Me 2,4-F2-PhNH- 0.29 >25 91
6i H F H F Me 1-Piperidinyl >25 >25 1
6j H F H F Me 4-Morpholinyl >25 >25 1
6k H F H F Me n-ButylNH- >25 >25 1
6l H F H F Me 3,4-Cl2-PhCH2O- 7.8 >25 3
6m H F H F Me 2,4-F2-PhCH2NH- 5.9 >25 3
6n H F H F Me 4-F-PhCH2NH- 17.6 >25 1
6o H F H F Me 4-MeO-PhCH2NH- >25 >25 1
6p H F H F Me 3-MeO-PhNH- >25 >25 1
6q H F H F Me 4-MeO-PhNH- >25 >25 1
6r H F H F Me 4-Br-PhNH- 1.13 >25 28
6s H F H F Me 4-Cl-PhNH- 1.44 >25 22
6t H F H F Me 2,3,4-F3-PhNH- 0.53 >25 48
6u H F H F i-Pr 2,3,4-F3-PhNH- 0.086 ± 0.041d >25 500
6v H F H F i-Pr 2,4-F2-PhNH- 0.79 >25 45
6w Cl Cl H Cl i-Pr 2,3,4-F3-PhNH- 0.100 ± 0.023d 6.4 77
6x Cl H H Cl i-Pr 2,3,4-F3-PhNH- 0.166 ± 0.067d 10.89 ± 4.29d 9
6y Cl Cl F Cl i-Pr 2,4-F2-PhNH- 0.129 ± 0.026d >25 231
6z H Cl H CF3 i-Pr 2,4-F2-PhNH 0.13 7.3 144
a,b

IC50 and CC50 were derived from the results of at least two independent experiment in VERO.

c

SI (selectivity index) = CC50/IC50 for inhibiting MERS-CoV infection.

d

Mean ± SD of four independent tests.