Abstract
In the present study, novel imines (5-16) of para-aminosalicylic esters were prepared in good yield and purity for the investigation of their antimycobacterial properties in vitro. The chemical structures of the compounds were determined by IR, 1H-NMR, 13C-NMR, high resolution mass spectrometry and elemental analysis. Unlike para-aminosalicylic acid itself, these compounds are thermally stable and displayed activity in two models using pathogenic strains of Mycobacterium tuberculosis. Compound 5, bearing an ortho-hydroxybenzylidene unit, demonstrated promising activity in vitro and a range of cytotoxic and inhibitory properties that warrant further studies.
Keywords: Antimycobacterial properties, Drug design, Inhibitory concentrations, Iron acquisition, Mycobacterium tuberculosis. Para- Aminosalicylic acid.
Letters in Drug Design & Discovery
Title:Synthesis and Antitubercular Activities in Vitro of New p-Aminosalicylic Ester Imines
Volume: 11 Issue: 8
Author(s): Michael J. Hearn, Daniel J. Smaltz and Michael H. Cynamon
Affiliation:
Keywords: Antimycobacterial properties, Drug design, Inhibitory concentrations, Iron acquisition, Mycobacterium tuberculosis. Para- Aminosalicylic acid.
Abstract: In the present study, novel imines (5-16) of para-aminosalicylic esters were prepared in good yield and purity for the investigation of their antimycobacterial properties in vitro. The chemical structures of the compounds were determined by IR, 1H-NMR, 13C-NMR, high resolution mass spectrometry and elemental analysis. Unlike para-aminosalicylic acid itself, these compounds are thermally stable and displayed activity in two models using pathogenic strains of Mycobacterium tuberculosis. Compound 5, bearing an ortho-hydroxybenzylidene unit, demonstrated promising activity in vitro and a range of cytotoxic and inhibitory properties that warrant further studies.
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Cite this article as:
Hearn J. Michael, Smaltz J. Daniel and Cynamon H. Michael, Synthesis and Antitubercular Activities in Vitro of New p-Aminosalicylic Ester Imines, Letters in Drug Design & Discovery 2014; 11 (8) . https://dx.doi.org/10.2174/1570180811666140516233652
DOI https://dx.doi.org/10.2174/1570180811666140516233652 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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