期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 1, 页码 411-422出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.09.044
关键词
Cascade reactions; Isatin; Sarcosine; Phenylglycine; Spiropyrrolidines; Anti-tubercular activity
资金
- Department of Science and Technology, New Delhi [SR/S1/OC-70/2006]
- IRHPA
- FIST
- University Grants Commission, New Delhi
- DRS
- ASIST
- CSIR, New Delhi [36-155/2008]
One-pot three-component domino reactions of cyclic mono ketones, isatin and sarcosine/phenylglycine furnishing highly functionalised dispiropyrrolidines in moderate yields are described. The reaction when performed with cyclic amino acid, proline resulted in the dimerization of azomethine ylides. These compounds have been screened for their in vitro activity against Mycobacterium tuberculosis H37Rv (MTB) using agar dilution method. Among thirty eight compounds screened, 1-methyl-pyrrolo(spiro[2.3']-5-bromooxindole)spiro[3.2]-1- nitrosotetrahydro-4(1H)-pyridinone (4t) was found to be the most active with MIC of 1.98 mu M against MTB and was 3.86 and 25.64 times more potent than the standard first line TB drugs, ethambutol and pyrazinamide respectively. (C) 2009 Elsevier Masson SAS. All rights reserved.
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