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Issue 1, 2015
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Novel isoniazid–amidoether derivatives: synthesis, characterization and antimycobacterial activity evaluation

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Abstract

A series of isoniazid–amidoether derivatives was synthesized and screened for their antimycobacterial activity in vitro and in vivo. Most of the compounds exhibited potent in vitro activity against the Mycobacterium tuberculosis H37Rv strain with MIC99 values ranging from 0.39 to 3.125 μM. Five compounds were equally as potent as the reference compound isoniazid. The most active compound 3b, when evaluated for in vivo activity, exhibited mild reduction in the bacillary load in lungs. However it showed a better effect in spleens. All the compounds were also evaluated for their cytotoxicity against the THP-1 cell line and no toxicity was observed up to 50 μM concentrations. The calculated ADMET parameters for the compounds validated good pharmacokinetic properties, confirming that these compounds could be used as templates for the development of new anti-tuberculosis agents.

Graphical abstract: Novel isoniazid–amidoether derivatives: synthesis, characterization and antimycobacterial activity evaluation

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Supplementary files

Article information


Submitted
01 Jul 2014
Accepted
22 Sep 2014
First published
23 Sep 2014

Med. Chem. Commun., 2015,6, 131-137
Article type
Concise Article
Author version available

Novel isoniazid–amidoether derivatives: synthesis, characterization and antimycobacterial activity evaluation

D. Kumar, G. Khare, Beena, S. Kidwai, A. K. Tyagi, R. Singh and D. S. Rawat, Med. Chem. Commun., 2015, 6, 131
DOI: 10.1039/C4MD00288A

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