Table 1.
| |||||
---|---|---|---|---|---|
compd | n | R | IC50 (nM) | Log Da | MWb |
2a | 9 | Me | >10,000 | −0.08 | 362.5 |
2b | 3 | Ph | 3,500 | 0.01 | 464.5 |
2c | 5 | Ph | 1021 ± 93.2 | 1.14 | 492.6 |
2d | 9 | 4-PhF | 345.6 ± 15.3 | 2.13 | 602.6 |
2e | 9 | Bn | 288.5 ± 35.2 | 1.37 | 590.8 |
2f | 9 | n-Bu | 194.2 ± 3.8 | 3.68 | 488.7 |
2g | 9 | Ph | 172.7 ± 4.0 | 1.67 | 548.7 |
2h | 9 | 2-PhMe | 143.4 ± 7.0 | −0.75 | 590.8 |
2i | 9 | C6H11 | 140.6 ± 0.7 | 4.50 | 566.8 |
2j | 9 | 4-PhOMe | 134.0 ± 1.7 | 3.19 | 638.7 |
| |||||
CQ | 66.93 ± 2.3 | 319.9 |
measured by 1-octanol–water partition at pH 7.4
molecular weights of lipocations 2 minus the counterion