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 journalArticle

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
Externally publishedYes

Fingerprint

Peptidomimetics
Cysteine Proteinase Inhibitors
Cysteine Proteases
Antimalarials
Plasmodium falciparum
Aldehydes
Scaffolds
falcipain
Bz-423

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Micale, N., Kozikowski, A. P., Ettari, R., Grasso, S., Zappalà, M., Jeong, J. J., ... Chishti, A. H. (2006). Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents. Journal of Medicinal Chemistry, 49(11), 3064-3067. https://doi.org/10.1021/jm060405f

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents. / Micale, Nicola; Kozikowski, Alan P.; Ettari, Roberta; Grasso, Silvana; Zappalà, Maria; Jeong, Jong Jin; Kumar, Ajay; Hanspal, Manjit; Chishti, Athar H.

In: Journal of Medicinal Chemistry, Vol. 49, No. 11, 01.06.2006, p. 3064-3067.

Research output: Contribution to journalArticle

Micale, N, Kozikowski, AP, Ettari, R, Grasso, S, Zappalà, M, Jeong, JJ, Kumar, A, Hanspal, M & Chishti, AH 2006, 'Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents', Journal of Medicinal Chemistry, vol. 49, no. 11, pp. 3064-3067. https://doi.org/10.1021/jm060405f
Micale N, Kozikowski AP, Ettari R, Grasso S, Zappalà M, Jeong JJ et al. Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents. Journal of Medicinal Chemistry. 2006 Jun 1;49(11):3064-3067. https://doi.org/10.1021/jm060405f
Micale, Nicola ; Kozikowski, Alan P. ; Ettari, Roberta ; Grasso, Silvana ; Zappalà, Maria ; Jeong, Jong Jin ; Kumar, Ajay ; Hanspal, Manjit ; Chishti, Athar H. / Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents. In: Journal of Medicinal Chemistry. 2006 ; Vol. 49, No. 11. pp. 3064-3067.
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