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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
  1. * Apparent permeability (PappA-B) across MDR1-transfected MDCK cell monolayers in the apical (A-B) direction. Units are 10-6 cm/s. % recovery is presented in brackets. ** Value for mefloquine is an average of n = 3 assays.