Synthesis and Antimalarial Bioassay of Quinine - Peptide Conjugates

Authors: Panda, Siva S.; Ibrahim, Mohamed A.; Kuecuekbay, Hasan; Meyers, Marvin J.; Sverdrup, Francis M.; El-Feky, Said A.; Katritzky, Alan R.; Chemical Biology & Drug Design; (2013); 10.1111/cbdd.12134

Amino acid and peptide conjugates of quinine were synthesized using microwave irradiation in 52-95% yields using benzotriazole methodology. The majority of these conjugates retain in vitro antimalarial activity with IC50 values below 100 nm, similar to quinine.