Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue -, Pages 416-423Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.04.021
Keywords
Antitubercular activity; Mycobacterium tuberculosis; Multi-drug resistant tuberculosis; 1,3-Dipolar cycloaddition; Pyrans; 1,2,4-Oxadiazoles
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Funding
- Research Center, College of Science, King Saud University
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Four-component reactions of (R)-1-(1-phenylethyl)tetrahydro-4(1H)-pyridinone, aromatic aldehydes and malononitrile in a 1:2:1 molar ratio in the presence of solid sodium ethoxide under solvent free conditions afforded an inseparable mixture of two diastereomeric 4(H)-pyrans in near quantitative yields. These compounds upon 1,3-dipolar cycloaddition with nitrile oxides furnished two enantiomerically pure 1,2,4-oxadiazoles in moderate yields, which were screened for in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB). Among the compounds screened, compound 10h was found to be the most active in vitro with a MIC value of 0.07 and 0.14 mu M against MTB and MDR-TB respectively. (C) 2012 Elsevier Masson SAS. All rights reserved.
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