Synthesis of quinoline coupled [1,2,3]-triazoles as a promising class of anti-tuberculosis agents.

Karthik Kumar, K.; Prabu Seenivasan, S.; Kumar, V.; Mohan Das, T.

Carbohydrate Research; 2011; 346; 2084-2090.          

Abstract: 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 m lg/mL, respectively.

Keywords: Quinoline derivatives; Click chemistry; Cu(I) catalysed; Anti-tubercular activity; Saccharide triazole derivatives; Mycobacterium tuberculosis H37Rv

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