Journal
CARBOHYDRATE RESEARCH
Volume 346, Issue 14, Pages 2084-2090Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.carres.2011.06.028
Keywords
Quinoline derivatives; Click chemistry; Cu(I) catalysed; Anti-tubercular activity; Saccharide triazole derivatives; Mycobacterium tuberculosis H37Rv
Funding
- CSIR, New Delhi
- UGC, New Delhi
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A series of quinoline coupled 1,2,3-triazoles compounds have been synthesized by 'click chemistry' from azidomethyl quinoline with different alkynes. The efficiency and fidelity of the Cu(I)-catalyzed azide-alkyne reaction are substantiated by good yields and exclusive formation of the expected 1,4-disubstituted triazole product. All the synthesized compounds were screened for anti-tubercular activity against Mycobacterium tuberculosis H37Rv by luciferase reporter phage (LRP) assay. Quinoline coupled triazole sugar hybrid. 20 is the most potent compound in the series with 76.41% and 78.37% reduction calculated based on percentage reduction in Relative Light Units at 5 and 25 mu g/mL, respectively. (C) 2011 Elsevier Ltd. All rights reserved.
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