Synthesis and Antimalarial Evaluation of Cyclicβ-Amino Acid-Containing Dipeptides

This paper describes an efficient synthesis and the antiparasitic evaluation of cyclic β-amino acid-containing dipeptides 3.1-3.6 and 4.1-4.5. The antimalarial properties of all these dipeptides have been evaluated in vitro against Plasmodium falciparum and in vivo against Plasmodium berghai. Compounds 4.4 and 4.5 have been found to be very effective in this respect, with IC(50 )values of 3.87 and 3.64 μg/mL in the in vitro test, while 4.5 has also been found to be active in the in vivo evaluation.