title: Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.
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.
authors.affiliation: Dipartimento Farmaco-Chimico, University of Messina, Viale Annunziata, 98168 Messina, Italy. rettari@pharma.unime.it
authors.forename: Roberta
authors.initials: R
authors.lastname: Ettari
authors.forename: Maria
authors.initials: M
authors.lastname: Zappalà
authors.forename: Nicola
authors.initials: N
authors.lastname: Micale
authors.forename: Tanja
authors.initials: T
authors.lastname: Schirmeister
authors.forename: Christoph
authors.initials: C
authors.lastname: Gelhaus
authors.forename: Matthias
authors.initials: M
authors.lastname: Leippe
authors.forename: Astrid
authors.initials: A
authors.lastname: Evers
authors.forename: Silvana
authors.initials: S
authors.lastname: Grasso
mesh_terms: D003546:Cysteine Endopeptidases / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000201:enzymology*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013379:Substrate Specificity
chemical_list: D010455:Peptides; D011480:Protease Inhibitors; D003546:Cysteine Endopeptidases; C416224:falcipain 2; C446033:rhodesain