- The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
European journal of medicinal chemistry (2012-10-16)
Matshawandile Tukulula, Susan Little, Jiri Gut, Philip J Rosenthal, Baojie Wan, Scott G Franzblau, Kelly Chibale
PMID23064162
摘要
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, 4.12b and 4.12d, also showed 94 and 98% growth inhibitory activity against non-replicating and replicating Mycobacterium tuberculosis strains, respectively.
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