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
- PMC6565474
Electronic International Standard Serial Number (EISSN)
- 1364-548X
International Standard Serial Number (ISSN)
- 1359-7345
Digital Object Identifier (DOI)
- 10.1039/c9cc01689a
Language
- eng