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

Cited Authors

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

Published Date

  • June 2019

Published In

Volume / Issue

  • 55 / 49

Start / End Page

  • 7009 - 7012

PubMed ID

  • 31119221

Pubmed Central ID

  • 31119221

Electronic International Standard Serial Number (EISSN)

  • 1364-548X

International Standard Serial Number (ISSN)

  • 1359-7345

Digital Object Identifier (DOI)

  • 10.1039/c9cc01689a

Language

  • eng