Table 1.

Structure-activity relationships in vitro

Core structureEmbedded Image
Embedded Image
Embedded Image
Embedded Image
R2 substituentR1 = H
R1 = F
R1 = H
R1 = F
R1 = H
R1 = F
R1 = H
R1 = F
GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50GI50, μmol/LTMZ PF50
Embedded Image10.6 ± 2.77.4 ± 0.215.3 ± 3.95.1 ± 0.8>204.7 ± 0.411.1 ± 29.2 ± 1.411.8 ± 1.48.1 ± 2.2
Embedded Image41.3 ± 4.64 ± 0.910.9 ± 38 ± 0.511.2 ± 1.85.5 ± 0.8>204.6 ± 0.68.9 ± 35.3 ± 1.59.3 ± 0.911.5 ± 1.017 ± 4.73.8 ± 0.820 ± 0.33.4 ± 0.5
Embedded Image10.8 ± 3.98.7 0.210 ± 2.66.3 ± 2.8>205.2 ± 1.49.7 ± 2.37.8 ± 1.711.8 ± 1.210.8 ± 0.5
Embedded Image13.9 ± 1.39.4 ± 0.811.8 ± 0.76.4 ± 3.521.1 ± 3.48.4 ± 211.4 ± 2.011.3 ± 0.516.6 ± 3.29.9 ± 1.7