Table 4. Structures of Tested Quinolines and Naphthyridinesa.
compound | T. b. brucei EC50 [nM] | LM CLint M/R/H [μL/min/mg] | MDCK-MDR1 A to B (ER) [10–6 cm/s] |
---|---|---|---|
16 | 37 | 43/43/<25 | 7.5 (1.0) |
17 | 94 | 87/<25/<25 | 13.2 (0.8) |
18 | 40 | 151/52/<25 | 20.0 (0.6) |
19 | 95 | 51/46/<25 | 18.2 (0.7) |
20 | 14 | 588/59/40 | 9.2 (0.5) |
21 | 53 | 414/62/55 | 12.4 (0.6) |
Details on the biochemical and cellular assay as well as on clearance (Clint) and permeability (MDCK-MDR1) can be found in the Experimental Section.