Format

Send to

Choose Destination
Bioorg Med Chem. 2010 Jul 15;18(14):4928-38. doi: 10.1016/j.bmc.2010.06.010. Epub 2010 Jun 10.

Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.

Author information

1
Dipartimento Farmaco-Chimico, UniversitĂ  di Messina, Viale Annunziata, 98168 Messina, Italy.

Abstract

Herein we report the synthesis of a series of novel constrained peptidomimetics 2-10 endowed with a dipeptide backbone (D-Ser-Gly) and a vinyl ester warhead, structurally related to a previously identified lead compound 1, an irreversible inhibitor of falcipain-2, the main haemoglobinase of lethal malaria parasite Plasmodium falciparum. The new compounds were evaluated for their inhibition against falcipain-2, as well as against cultured P. falciparum. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense.

PMID:
20598553
DOI:
10.1016/j.bmc.2010.06.010
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center