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Eur J Med Chem. 2010 Jul;45(7):3228-33. doi: 10.1016/j.ejmech.2010.04.003. Epub 2010 Apr 14.

Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.

Author information

1
Dipartimento Farmaco-Chimico, University of Messina, Viale Annunziata, 98168 Messina, Italy. rettari@pharma.unime.it

Abstract

This paper describes the synthesis of novel peptidomimetics bearing a protected aspartyl aldeyde warhead leading to the thioacylals 2a,b and the acylals 3a,b. Compounds 2a and 3a proved to possess an increased antiplasmodial activity with respect to the parent molecule 1. Furthermore thioacylal 2a can be considered as a promising trypanocidal agent.

PMID:
20434817
DOI:
10.1016/j.ejmech.2010.04.003
[Indexed for MEDLINE]

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