The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
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.
Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Matshawandile
M
Tukulula
Susan
S
Little
Jiri
J
Gut
Philip J
PJ
Rosenthal
Baojie
B
Wan
Scott G
SG
Franzblau
Kelly
K
Chibale
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001681:Biological Assay; D001812:Blood-Brain Barrier / Q000378:metabolism; D003198:Computer Simulation; D015195:Drug Design; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D015767:Mefloquine / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008954:Models, Biological; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D011803:Quinine / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000634:Aminoquinolines; D000981:Antiprotozoal Agents; D000995:Antitubercular Agents; D013777:Tetrazoles; D011803:Quinine; D015767:Mefloquine