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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.

Publication ,  Journal Article
Szamosvári, D; Sylvester, K; Schmid, P; Lu, K-Y; Derbyshire, ER; Böttcher, T
Published in: Chemical communications (Cambridge, England)
June 2019

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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Published In

Chemical communications (Cambridge, England)

DOI

EISSN

1364-548X

ISSN

1359-7345

Publication Date

June 2019

Volume

55

Issue

49

Start / End Page

7009 / 7012

Related Subject Headings

  • Toxoplasma
  • Structure-Activity Relationship
  • Quinolones
  • Plasmodium
  • Parasitic Sensitivity Tests
  • Organic Chemistry
  • Molecular Structure
  • Humans
  • Dose-Response Relationship, Drug
  • Cyclization
 

Citation

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Szamosvári, D., Sylvester, K., Schmid, P., Lu, K.-Y., Derbyshire, E. R., & Böttcher, T. (2019). 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. Chemical Communications (Cambridge, England), 55(49), 7009–7012. https://doi.org/10.1039/c9cc01689a
Szamosvári, Dávid, Kayla Sylvester, Philipp Schmid, Kuan-Yi Lu, Emily R. Derbyshire, and Thomas Böttcher. “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.Chemical Communications (Cambridge, England) 55, no. 49 (June 2019): 7009–12. https://doi.org/10.1039/c9cc01689a.
Szamosvári D, Sylvester K, Schmid P, Lu K-Y, Derbyshire ER, Böttcher T. 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. Chemical communications (Cambridge, England). 2019 Jun;55(49):7009–12.
Szamosvári, Dávid, et al. “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.Chemical Communications (Cambridge, England), vol. 55, no. 49, June 2019, pp. 7009–12. Epmc, doi:10.1039/c9cc01689a.
Szamosvári D, Sylvester K, Schmid P, Lu K-Y, Derbyshire ER, Böttcher T. 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. Chemical communications (Cambridge, England). 2019 Jun;55(49):7009–7012.
Journal cover image

Published In

Chemical communications (Cambridge, England)

DOI

EISSN

1364-548X

ISSN

1359-7345

Publication Date

June 2019

Volume

55

Issue

49

Start / End Page

7009 / 7012

Related Subject Headings

  • Toxoplasma
  • Structure-Activity Relationship
  • Quinolones
  • Plasmodium
  • Parasitic Sensitivity Tests
  • Organic Chemistry
  • Molecular Structure
  • Humans
  • Dose-Response Relationship, Drug
  • Cyclization