Synthesis and Antimalarial Evaluation of Cyclic β-Amino Acid-Containing Dipeptides

Abstract

This paper describes an efficient synthesis and the antiparasitic evaluation ofcyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial propertiesof all these dipeptides have been evaluated in vitro against Plasmodium falciparum and invivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be veryeffective in this respect, with IC50 values of 3.87 and 3.64 μg/mL in the in vitro test, while4.5 has also been found to be active in the in vivo evaluation.

Keywords

• β-Lactam
• β-amino acid
• antimalarial
• Plasmodium falciparum
• Plasmodium berghai