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. 2022 Aug 22;65(17):11776–11787. doi: 10.1021/acs.jmedchem.2c00791

Table 4. Structures of Tested Quinolines and Naphthyridinesa.

graphic file with name jm2c00791_0007.jpg

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)
a

Details on the biochemical and cellular assay as well as on clearance (Clint) and permeability (MDCK-MDR1) can be found in the Experimental Section.