Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 9, Pages 2035-2043Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.03.018
Keywords
Hydroxynaphthalene-2-carboxanilides; In vitro antimycobacterial activity; MTT assay; In vitro cytotoxicity; Structure-activity relationships
Funding
- IGA VFU Brno [304/2015/FaF, 322/2015/FaF, 37/2014/FaF, 108/2013/FaF]
- Slovak Grant Agency [VEGA 1/0972/12]
- Irish Department of Agriculture Fisheries and Food (FIRM) [08RDCIT601, 08RDCIT617]
- [APVV-0061-11]
- [CZ.1.07/2.3.00/30.0053]
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In this study, a series of twenty-two ring-substituted 6-hydroxynaphthalene-2-carboxanilides was prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Mycobacterium tuberculosis H37Ra, Mycobacterium avium complex and M. avium subsp. paratuberculosis. Derivatives substituted by trifluoromethyl, bromo, methyl and methoxy moieties in C-(3)' and C-(4)' positions of the anilide ring showed 2-fold higher activity against M. tuberculosis than isoniazid and 4.5-fold higher activity against M. avium subsp. paratuberculosis than rifampicin. 6-Hydroxy-N-(2-methylphenyl) naphthalene-2-carboxamide had MIC = 29 mu M against M. avium complex. A significant decrease of mycobacterial cell metabolism (viability of M. tuberculosis H37Ra) was observed using MTT assay. Screening of the cytotoxicity of the most effective antimycobacterial compounds was performed using the THP-1 cells, and no significant lethal effect was observed. The structure-activity relationships are discussed. (C) 2015 Elsevier Ltd. All rights reserved.
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