Evaluation of Structurally Related 3-Substituted 4-Amino-2-arylquinolines and 2-Aryl-4-methoxyquinolines for Potential Antimycobacterial Activity
Keywords:antimycobacterial activity, Mycobacterium tuberculosis, immunomodulation, 2-aryl-4-methoxyquinolines, 4-amino-2-arylquinolines
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 Âµg/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 â‰¥5.0â‰¤20.0 Âµg/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.
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