Series of structurally related 2-aryl-4-(amino/methoxy)quinoline derivatives were evaluated for potential antimycobacterial activity against Mycobacterium tuberculosis strain H37Rv. A complete inhibition of a drug sensitive strain of M. tuberculosis was observed at 20.0 µg/ml for 4-amino-2-(4-chlorophenyl)quinoline 3b, 4-amino-3-iodo-2-(4-methoxyphenyl)quinoline 5d, 4-amino-2,3-diphenylquinoline 6a, 4-amino-2-(4-fluorophenyl)-3-phenylquinoline 6b and 4-amino-2-(4-methoxyphenyl)-3-phenylquinoline 6d. These derivatives were further evaluated for activity against a multidrug resistant strain of M. tuberculosis. The minimum inhibitory concentration (MIC) against a two drug-resistant strain was found to be ≥5.0≤20.0 µg/ml. Systems 6a and 6b were, in turn, subjected to cytotoxicity assay using U937 human macrophages and their intracellular antimycobacterial activity was also determined. Moreover, these two 4-amino-2,3-diarylquinoline derivatives were also investigated for their immune modulatory effect according to Th1 and Th2-subset cytokines.
via The International Arabic Journal of Antimicrobial Agents http://imedpub.com/ojs/index.php/IAJAA/article/view/526