Figure 11.
Further exploration of the anthranilamide class of compounds where the phenoxyaniline substituent has been replaced with a diphenylmethylpiperazine moiety [51].
Compd. No. | R1 | R2 | Radioligand Displacement Assay IC50 (μM) | SH-SY5Y Neuroblastoma Cells IC50 (μM) | HEK293 hCav2.2 + β3 + α2δ1 IC50 (μM) |
---|---|---|---|---|---|
25 | H | NH2 | 214 | 160 | 232 |
26 | H | N=C(NH2)2 | 12 | 206 | 299 |
27 | F | NH2 | 65 | 286 | 288 |
28 | F | N=C(NH2)2 | 16 | 156 | 156 |