title: Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.
abstract: The synthesis of a new class of peptidomimetics 1a-j, based on a 1,4-benzodiazepine scaffold and on a C-terminal aspartyl aldehyde building block, is described. Compounds 1a-j provided significant inhibitory activity against falcipains 2A and 2B (FP-2A and FP-2B), two cysteine proteases from Plasmodium falciparum.
authors.affiliation: Dipartimento Farmaco Chimico, University of Messina, Viale Annunziata, 98168, Messina, Italy. nmicale@pharma.unime.it
authors.forename: Nicola
authors.initials: N
authors.lastname: Micale
authors.forename: Alan P
authors.initials: AP
authors.lastname: Kozikowski
authors.forename: Roberta
authors.initials: R
authors.lastname: Ettari
authors.forename: Silvana
authors.initials: S
authors.lastname: Grasso
authors.forename: Maria
authors.initials: M
authors.lastname: Zappalà
authors.forename: Jong-Jin
authors.initials: JJ
authors.lastname: Jeong
authors.forename: Ajay
authors.initials: A
authors.lastname: Kumar
authors.forename: Manjit
authors.initials: M
authors.lastname: Hanspal
authors.forename: Athar H
authors.initials: AH
authors.lastname: Chishti
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry; D003546:Cysteine Endopeptidases / Q000737:chemistry; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D018716:Molecular Mimicry; D010455:Peptides / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000201:enzymology; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D015853:Cysteine Proteinase Inhibitors; D010455:Peptides; D001569:Benzodiazepines; D001224:Aspartic Acid; C006644:aspartic semialdehyde; D003546:Cysteine Endopeptidases; C416224:falcipain 2