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.\}",

year = "2006",

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doi = "10.1021/jm060405f",

language = "English (US)",

volume = "49",

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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.

UR - https://www.scopus.com/pages/publications/33744805804

UR - https://www.scopus.com/pages/publications/33744805804#tab=citedBy

U2 - 10.1021/jm060405f

DO - 10.1021/jm060405f

M3 - Article

C2 - 16722625

AN - SCOPUS:33744805804

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EP - 3067

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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