Jump to main content
Jump to site search

Issue 49, 2019
Previous Article Next Article

Close the ring to break the cycle: tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-a]quinolin-5-ones with potent anti-protozoal activity

Author affiliations

Abstract

Expanding the chemical space of quinolones led to a tandem quinolone-alkyne-cyclisation reaction allowing chemoselective control of the synthesis of tricyclic pyrrolo[1,2-a]quinolin-5-ones. Importantly, we discovered anti-protozoal activity against Plasmodium and Toxoplasma with specific potency of one of the compounds against the liver stage of the malaria parasite in the nanomolar range.

Graphical abstract: Close the ring to break the cycle: tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-a]quinolin-5-ones with potent anti-protozoal activity

Back to tab navigation

Supplementary files

Publication details

The article was received on 28 Feb 2019, accepted on 10 May 2019 and first published on 13 May 2019


Article type: Communication
DOI: 10.1039/C9CC01689A
Chem. Commun., 2019,55, 7009-7012

  •   Request permissions

    Close the ring to break the cycle: tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-a]quinolin-5-ones with potent anti-protozoal activity

    D. Szamosvári, K. Sylvester, P. Schmid, K. Lu, E. R. Derbyshire and T. Böttcher, Chem. Commun., 2019, 55, 7009
    DOI: 10.1039/C9CC01689A

Search articles by author

Spotlight

Advertisements