Table 2 Base structure and results of L1 assays for diamine (AA) derivatives against T. muris
| Compound | T. muris L1 assay | Cytotoxicity | Selectivity indexes | |||||
|---|---|---|---|---|---|---|---|---|---|
Compound identification | N | R1/R2 | R3 | % dead larvae (100 µM) | IC50 (µM) | Caco 2 CC50 (µM) | HepG2 CC50 (µM) | SI Caco2 | SI HepG2 |
AA16 | 13 | H/H | H | 0.00 | – | – | – | – | – |
AA17 | 17 | H/H | H | 9.80 | |||||
AA18 | 9 | H/H | Boc | 93.55 | 21.9 | 30.24 ± 1.56 | 25.20 ± 0.33 | 1.4 | 1.1 |
AA19 | 13 | H/H | Boc | 32.47 | – | – | – | – | – |
AA20 | 15 | H/H | Boc | 20.79 | – | – | – | – | – |
AA21 | 17 | H/H | Boc | 23.86 | – | – | – | – | – |
AA22 | 13 | Et/Et | H | 75.02 | – | – | – | – | – |
AA23 | 13 | H/Et | Boc | 87.49 | – | – | – | – | – |
AA24 | 13 | Et/Et | Boc | 61.85 | – | – | – | – | – |
AA25 | 13 | H/Bu | Boc | 28.98 | – | – | – | – | – |
AA26 | 13 | H/Hex | Boc | 12.91 | – | – | – | – | – |
