The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives

M Tukulula, S Little, J Gut, PJ Rosenthal, B Wan…

Index: Tukulula, Matshawandile; Little, Susan; Gut, Jiri; Rosenthal, Philip J.; Wan, Baojie; Franzblau, Scott G.; Chibale, Kelly European Journal of Medicinal Chemistry, 2012 , vol. 57, p. 259 - 267

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Citation Number: 16

Abstract

A series of new arylamino quinoline derivatives was designed based on the quinine and mefloquine scaffolds and evaluated in vitro for antiplasmodial and antimycobacterial activities. A number of these compounds exhibited significant activity against the drug- sensitive 3D7 and drug-resistant K1 strains of Plasmodium falciparum. Furthermore, two compounds, 4.12 b and 4.12 d, also showed 94 and 98% growth inhibitory activity against ...