Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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Synthesis and Antitubercular Activities in Vitro of New p-Aminosalicylic Ester Imines

Author(s): Michael J. Hearn, Daniel J. Smaltz and Michael H. Cynamon

Affiliation: Department of Chemistry, Wellesley College, Wellesley, Massachusetts 02481.

Keywords: Antimycobacterial properties, Drug design, Inhibitory concentrations, Iron acquisition, Mycobacterium tuberculosis. Para- Aminosalicylic acid.

Graphical Abstract:


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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Article Details

VOLUME: 11
ISSUE: 8
Page: [953 - 959]
Pages: 7
DOI: 10.2174/1570180811666140516233652