期刊
TETRAHEDRON LETTERS
卷 51, 期 49, 页码 6439-6443出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2010.09.128
关键词
1,3-Dipolar cycloaddition; Pyridinium ylides; Indolizines; Pyrrolo[2,1-a]isoquinolines; Domino; Three-component; Antimycobacterial; Mycobacterium tuberculosis
资金
- Department of Science and Technology, New Delhi [DST/INT/SPAIN/09]
- IRH
- University Grants Commission, New Delhi
The domino reactions of pyridine/isoquinoline, bromoacetonitrile/ethyl bromoacetate and a series of beta-nitrostyrenes in the presence of triethylamine afforded novel tri-/disubstituted indolizines and pyrrolo [2,1-a]isoquinolines regioselectively, presumably via substitution-dipole generation-1,3-dipolar cycloaddition-elimination and/or aromatisation sequence. In vitro screening of all the seventeen compounds synthesized against Mycobacterium tuberculosis H37Rv discloses that ethyl 2-(4-fluorophenyl)pyrrolo [2,1-a]isoquinoline-3-carboxylate displays maximum potency with minimum inhibitory concentration (MIC) of 1.0 mu M, being 7.6 and 4.7 times more potent than the standard first line TB drugs, ethambutol and ciprofloxacin, respectively. (C) 2010 Elsevier Ltd. All rights reserved.
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