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.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Derbyshire, Emily R.

Cited Authors

Szamosvári, D; Sylvester, K; Schmid, P; Lu, K-Y; Derbyshire, ER; Böttcher, T

Published Date

June 2019

Published In

Chemical Communications

Volume / Issue

55 / 49

Start / End Page

7009 - 7012

PubMed ID

31119221

Pubmed Central ID

PMC6565474

Electronic International Standard Serial Number (EISSN)

1364-548X

International Standard Serial Number (ISSN)

1359-7345

Digital Object Identifier (DOI)

10.1039/c9cc01689a

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