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. 2016 May 12;24(13):3035–3042. doi: 10.1016/j.bmc.2016.05.013

Table 1.

IC50 values of analogues against MERS and SARS 3CLpro

graphic file with name fx2_lrg.jpg

Sl. No. R1 R2 R3 R4 SARS IC50 (μM) MERS IC50 (μM)
3a COOH Cl CH3 3-COOH >50 >50
3b COOH Cl CF3 3-COOH >50 >50
3c COOH H CF3 3-COOH >50 >50
3d COOH Cl Ph 3-COOH 44.7 ± 5.1 >50
3e COOH Cl CH3 H >50 >50
3f COOH Cl Ph H 16.4 ± 0.7 12.2 ± 2.2
3g COOH Cl Ph 4-F 20.2 ± 0.3 10.1 ± 1.8
3h COOH Cl Ph 4-CH(CH3)2 6.0 ± 1.2 7.3 ± 2.1
3i COOH Cl Ph 4-CH(CH3)3 5.8 ± 1.5 7.4 ± 2.2
3j H H Ph H >50 >50
3k H H Ph COOH 6.4 ± 1.2 5.8 ± 1.6
3l H H CH3 COOH >50 >50
3m COOH H Ph H 41.2 ± 9.5 30.3 ± 4.5
3n COOH H Ph 4-F 37.5 ± 0.7 >50
3o COOH H Ph 4-CH(CH3)2 11.7 ± 2.5 8.9 ± 1.8
3p COOH H Ph 4-CH(CH3)3 8.6 ± 2.1 7.7 ± 2.2
3q COOH H Ph 4-CN 18.7 ± 4.5 9.6 ± 1.6
3r COOH H Ph 4-OCH3 30.7 ± 5.8 8.9 ± 1.8
3s No ring A Ph COOH >50 >50