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Letters in Drug Design & Discovery
ISSN (Print): 1570-1808
ISSN (Online): 1875-628X
Epub Full Text Article
DOI: 10.2174/1570180811666140516233652      Price:  $95









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

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Author(s): Michael J. Hearn, Daniel J. Smaltz and Michael H. Cynamon
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:
para-Aminosalicylic acid, Antimycobacterial properties, Drug design, Inhibitory concentrations, Iron acquisition, Mycobacterium tuberculosis
Affiliation:
Department of Chemistry Wellesley College Wellesley Massachusetts 02481 USA.