Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 1, Pages 350-353Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.107
Keywords
Antitubercular activity; Mycobacterium tuberculosis; Multi-drug resistant tuberculosis; Azomethine ylide; 1,3-Dipolar cycloaddition; Spiro-pyrrolothiazoles
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Funding
- Department of Science and Technology, New Delhi [SR/S1/OC-70/2006]
- IRHPA
- FIST
- University Grants Commission, New Delhi
- DRS
- ASIST programs
- Council of Scientific and Industrial Research, New Delhi
- [36-155/2008 (SR)]
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The 1,3-dipolar cycloaddition of azomethine ylides derived from substituted isatins and 1,3-thiazolane-4-carboxylic acid to a series of 1-methyl-3,5-bis[(E)-arylmethylidene]-tetrahydro-4(1H)-pyridinones afforded novel spiro-pyrrolothiazoles chemo-, regio- and stereoselectively in quantitative yields. These compounds were screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) and multi-drug resistant M. tuberculosis (MDR-TB) using agar dilution method. Among the synthesized compounds, spiro[5.3 '']-5 ''-nitrooxindole-spiro-[6.3']-1'-methyl-5'-(2,4-di-chlorophenylmethylidene)tetrahydro-4'(1H)-pyridinone-7-(2,4-dichlorophenyl)tetra-hydro-1H-pyrrolo[1,2-c][1,3]thiazole (9k) was found to be the most active with a minimum inhibitory concentration (MIC) of 0.6 mu M against MTB and MDR-TB. (C) 2009 Elsevier Ltd. All rights reserved.
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