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. 2022 Nov 5;12(12):342. doi: 10.1007/s13205-022-03408-8

Table 1.

The structures of isoxazole derivatives and the IC50 values against COX enzymes

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Name R1 R2 IC50 COX-1 (µM) IC50 COX-2 (µM) Selectivity index
A1 H H 0.839 ± 0.04 1.214 ± 0.78 0.69
A2 H 3-OCH3, 4-OCH3, 5-OCH3 0.269 ± 0.17 3.949 ± 1.02 0.07
A3 H 3- OCH3, 5-OCH3 0.122 ± 0.11 0.310 ± 0.25 0.39
A4 H 3-OCH3, 4-OCH3 0.076 ± 0.06 0.258 ± 0.28 0.29
A5 H 4-t-butyl 0.312 ± 0.16 0.486 ± 0.01 0.65
A6 4-F H 0.140 ± 0.05 0.218 ± 0.11 0.6418
A7 4-F 3-OCH3, 4-OCH3, 5-OCH3 0.350 ± 0.05 0.346 ± 0.24 1.0113
A8 4-F 3-OCH3,5-OCH3 0.317 ± 0.02 0.878 ± 0.47 0.3618
A9 4-F 3-OCH3, 4-OCH3 0.335 ± 0.07 0.829 ± 0.15 0.4047
A10 4-F 4-t-butyl 0.126 ± 0.10 0.370 ± 0.08 0.3403
A11 4-F 2-OCH3, 4-Cl, 5-OCH3 0.478 ± 0.21 0.334 ± 0.03 0.5604
A12 2-Cl 3-OCH3,5-OCH3 0.413 ± 0.19 0.293 ± 0.11 1.4117
A13 2-Cl 3-OCH3, 4-OCH3 0.064 ± 0.02 0.013 ± 0.01 4.6341
A14 2-Cl 2-OCH3, 5-OCH3 0.077 ± 0.01 0.376 ± 0.21 0.2066
B1 2-Cl 1.210 ± 0.55 0.856 ± 0.15 1.414454
B2 4-F 0.702 ± 0.28 0.033 ± 0.07 20.72017
B3 H 0.668 ± 0.08 1.040 ± 0.85 0.642553
Ketoprofen 0.043 ± 0.02 0.066 ± 0.05 0.643249
Celecoxib 1.479 ± 0.47 0.004 ± 0.003 369.75