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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

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.

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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, Accepted Manuscript

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    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. Szamosvari, K. Sylvester, P. Schmid, K. Lu, E. Derbyshire and T. Böttcher, Chem. Commun., 2019, Accepted Manuscript , DOI: 10.1039/C9CC01689A

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