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Issue 52, 2016, Issue in Progress
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Synthesis and anti-tubercular activity of fused thieno-/furo-quinoline compounds

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Abstract

A simple route for preparation of 4-substituted thieno/furo[2,3-c]quinoline compounds is reported in this paper. These compounds were synthesized by using Suzuki coupling between appropriate boronic acid and 2-iodoaniline, followed by reaction with diverse aldehydes in the presence of a catalytic amount of FeCl3. Naphthyridine analogues were also prepared in order to demonstrate the efficacy of the developed method. Further anti-tubercular activity screening of the molecules was undertaken, wherein compounds bearing a fused furo[2,3-c][1,8]naphthyridine skeleton displayed highest activity. The best MIC (minimum inhibitory concentration) value of 5.6 μmol was obtained for 4-(4-methoxyphenyl)furo[2,3-c][1,8]naphthyridine, which is found to be superior to the existing first line anti-tubercular drug ethambutol (7.6 μmol).

Graphical abstract: Synthesis and anti-tubercular activity of fused thieno-/furo-quinoline compounds

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Supplementary files

Article information


Submitted
03 Feb 2016
Accepted
04 May 2016
First published
06 May 2016

RSC Adv., 2016,6, 46073-46080
Article type
Paper

Synthesis and anti-tubercular activity of fused thieno-/furo-quinoline compounds

M. Akula, P. Yogeeswari, D. Sriram, M. Jha and A. Bhattacharya, RSC Adv., 2016, 6, 46073
DOI: 10.1039/C6RA03187K

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