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Issue 49, 2019
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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

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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

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Article information


Submitted
28 Feb 2019
Accepted
10 May 2019
First published
13 May 2019

Chem. Commun., 2019,55, 7009-7012
Article type
Communication

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

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