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

doi:10.1021/jm060405f

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 journal › Article › peer-review

67 Scopus citations

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 language	English (US)
Pages (from-to)	3064-3067
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	49
Issue number	11
DOIs	https://doi.org/10.1021/jm060405f
State	Published - Jun 1 2006
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm060405f

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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.",

author = "Nicola Micale and Kozikowski, {Alan P.} and Roberta Ettari and Silvana Grasso and Maria Zappal{\`a} and Jeong, {Jong Jin} and Ajay Kumar and Manjit Hanspal and Chishti, {Athar H.}",

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doi = "10.1021/jm060405f",

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T1 - Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents

AU - Micale, Nicola

AU - Kozikowski, Alan P.

AU - Ettari, Roberta

AU - Grasso, Silvana

AU - Zappalà, Maria

AU - Jeong, Jong Jin

AU - Kumar, Ajay

AU - Hanspal, Manjit

AU - Chishti, Athar H.

PY - 2006/6/1

Y1 - 2006/6/1

N2 - 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.

AB - 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.

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DO - 10.1021/jm060405f

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JO - Journal of medicinal chemistry

JF - Journal of medicinal chemistry

IS - 11

ER -

Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents

Abstract

ASJC Scopus subject areas

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