Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents

Nicola Micale, Alan P. Kozikowski, Roberta Ettari, Silvana Grasso, Maria Zappalà, Jong Jin Jeong, Ajay Kumar, Manjit Hanspal, Athar H. Chishti

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish (US)
Pages (from-to)3064-3067
Number of pages4
JournalJournal of medicinal chemistry
Volume49
Issue number11
DOIs
StatePublished - Jun 1 2006

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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