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Original Article

J App Pharm Sci. 2018; 8(8): 107-115

Novel synthetic analogues of Fluoxetine as potent and selective anti-TB agents

M. Murali Krishna Kumar, K. Madhavi, T. Mohan, K. Purna Nagasree, G. P. V. Sangeeta.


We have recently identified potent anti TB activity in several CNS drugs. Most prominently, the phenothiazine antipsychotics (Thioridazine-MIC 3.125μg/mL) and anti-depressant drugs (sertraline-MIC 1.6μg/mL) have shown anti TB activity against Mycobacterium tuberculosis H37Rv. In continuation, we have synthesized a series of 1-(3-aryloxy-3-phenylpropyl) amine analogues of fluoxetine with a view to optimize its anti TB activity. Identities of the synthesized compounds were confirmed on the basis of FTIR, 1H NMR and mass spectral analysis. Further, all synthesized compounds and intermediates were screened for antimicrobial activity using serial dilution method. Antitubercular activities of these compounds were performed by using Microplate Alamar Blue Assay (MABA) method. Among the synthesized compounds, 1-(3-(4-fluorophenoxy)-3-phenylpropyl)piperidine(AM3e) has shown highest anti TB activity (MIC 1.6μg/mL) against MtbH37Rv and is free from antibacterial/antifungal activity (MIC >100μg/mL).

Key words: Acetophenone mannich bases, fluoxetine, antitubercular activity, drug repurposing

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