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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Chemical Communications : ChemComm. 2019, 55(49), pp. 7009-7012. ISSN 0009-241X. eISSN 1364-548X. Available under: doi: 10.1039/C9CC01689A
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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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SZAMOSVARI, David, Kayla SYLVESTER, Philipp SCHMID, Kuan-Yi LU, Emily R. DERBYSHIRE, Thomas BÖTTCHER, 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. In: Chemical Communications : ChemComm. 2019, 55(49), pp. 7009-7012. ISSN 0009-241X. eISSN 1364-548X. Available under: doi: 10.1039/C9CC01689ABibTex
@article{Szamosvari2019-06-13Close-45977, year={2019}, doi={10.1039/C9CC01689A}, title={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}, number={49}, volume={55}, issn={0009-241X}, journal={Chemical Communications : ChemComm}, pages={7009--7012}, author={Szamosvari, David and Sylvester, Kayla and Schmid, Philipp and Lu, Kuan-Yi and Derbyshire, Emily R. and Böttcher, Thomas} }
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