Table 3 Metabolic stability, drug-drug interaction and permeability screening results for mefloquine and interesting next generation quinoline methanols
From: Anti-malarial activity of a non-piperidine library of next-generation quinoline methanols
WR# | Half-life in mouse micro (min) | IC50 1A2 (uM) | IC50 2C9 (uM) | IC50 2C19 (uM) | IC50 2D6 (uM) | IC50 3A4 (uM) | PappA-BMDCK-MDR1 in cells(% recovery)* |
|---|---|---|---|---|---|---|---|
MQ | > 60 | > 40 | 14 | 18 | 5.1 | 19 | 9.4 (< 40)** |
308245 | > 60 | 1.8 | > 40 | 33 | 7.4 | 26 | 24 (59) |
308255 | 25 | 1.5 | 25 | 25 | 2.9 | 18 | NT |
308257 | > 60 | 3.9 | 37 | 26 | 1.9 | > 40 | 25 (69) |
308266 | 22 | 2.4 | 12 | 7.6 | 1.4 | 5.7 | NT |
308278 | 10 | 3.5 | 6.3 | 3.6 | 1.4 | 16 | 38 (54) |
308396 | > 60 | 5.4 | 14 | 5.8 | 0.7 | 3.3 | 8.4 (18) |
308446 | 13 | > 40 | 16 | 14 | 9.1 | > 40 | NT |
398387 | 20 | 2.1 | 11 | 7 | 2 | > 40 | 18 (42) |
308388 | 16 | 1.2 | 13 | 3.4 | 0.8 | 33 | NT |
308413 | 19 | 26 | 19 | 5.8 | 1 | > 40 | NT |