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Eur J Med Chem ; 74: 333-9, 2014 Mar 03.
Article in English | MEDLINE | ID: mdl-24486416

ABSTRACT

A series of seventeen new 6-(4-substitutedpiperazin-1-yl)phenanthridine derivatives were designed, synthesized, and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv by Microplate Alamar Blue Assay and most active compounds were tested for cytotoxicity studies against mouse macrophage cell lines (RAW264.7). Among the tested compounds, ten compounds exhibited significant activity against the growth of M. tuberculosis (MIC ranging from 1.56 to 6.25 µg/mL). In particular, compounds 5e, 5j and 5k displayed excellent activity against the growth of M. tuberculosis (MIC 1.56 µg/mL). The selectivity index values were found to be >25, indicating compounds likeliness in drug development for tuberculosis. The structure of 5k is substantiated by X-ray crystallographic study. Structure-activity correlation indicates the importance of substituent at 4th position of piperazinyl phenanthridine ring.


Subject(s)
Antitubercular Agents/chemical synthesis , Antitubercular Agents/pharmacology , Phenanthridines/chemical synthesis , Phenanthridines/pharmacology , Animals , Cell Line , Crystallography, X-Ray , Macrophages/drug effects , Magnetic Resonance Spectroscopy , Mice , Microbial Sensitivity Tests , Mycobacterium tuberculosis/drug effects , Mycobacterium tuberculosis/growth & development , Spectrometry, Mass, Electrospray Ionization
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