Table 1 Base structure and results of L1 assays for aminoalcohol (AO) derivatives against T. muris
| Compound | T. muris L1 assay | Cytotoxicity | Selectivity Indexes | |||||
|---|---|---|---|---|---|---|---|---|---|
Compound identification | N | R1 | R2 | % dead larvae (100 µM) | IC50 µM | Caco 2 CC50 (µM) | HepG2 CC50 (µM) | SI Caco2 | SI HepG2 |
AO1 | 9 | H | H | 65.09 | – | – | – | – | – |
AO2 | 13 | H | H | 78.36 | – | – | – | – | – |
AO3 | 15 | H | H | 36.47 | – | – | – | – | – |
AO4 | 15 | H | Et | 85.29 | – | – | – | – | – |
AO5 | 17 | H | Et | 97.04 | 25.6 | 13.01 ± 0.27 | 9.13 ± 0.56 | < 1.0 | < 1.0 |
AO6 | 13 | H | Bu | 74.44 | – | – | – | – | – |
AO7 | 13 | H | Hex | 53.25 | – | – | – | – | – |
AO8 | 13 | H | Dec | 23.66 | – | – | – | – | – |
AO9 | 13 | H | Boc | 29.63 | – | – | – | – | – |
AO10 | 9 | Bn | H | 61.27 | – | – | – | – | – |
AO11 | 13 | Bn | H | 97.83 | 17.5 | > 20 | 6.48 ± 0.18 | > 1.1 | < 1.0 |
AO12 | 15 | Bn | H | 25.55 | – | – | – | – | – |
AO13 | 17 | Bn | H | 27.23 | – | – | – | – | – |
| Compound | T. muris L1 assay | Cytotoxicity | Selectivity Indexes | ||||
|---|---|---|---|---|---|---|---|---|
Compound identification | N | R1 | % dead larvae (100 µM) | IC50 µM | Caco 2 CC50 (µM) | HepG2 CC50 (µM) | SI Caco2 | SI HepG2 |
AO14 | 4 | H | 96.60 | 3.3 | > 15 | 13.68 ± 1.13 | > 4.5 | 4.1 |
AO15 | 6 | H | 100.00 | 46.0 | 32.79 ± 1.28 | 8.74 ± 1.65 | < 1.0 | < 1.0 |
