Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors

Edite Verissimo; Neil Berry; Peter Gibbons; M. Lurdes S. Cristiano; Philip J. Rosenthal; Jiri Gut; Steve Ward; Paul M. O'Neill

doi:10.1016/j.bmcl.2008.05.068

Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors

Edite Verissimo
, Neil Berry
, Peter Gibbons
, M. Lurdes S. Cristiano
, Philip J. Rosenthal
, Jiri Gut
, Steve Ward
, Paul M. O'Neill

Tropical Disease Biology

Research output: Contribution to journal › Article › peer-review

73 Citations (Scopus)

Abstract

The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. (C) 2008 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	4210-4214
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2008.05.068
Publication status	Published - 15 Jul 2008

Keywords

Cysteine protease
Falcipain-2
Malaria
Peptidomimetic
Plasmodium falciparum

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10.1016/j.bmcl.2008.05.068

Cite this

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title = "Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors",

abstract = "The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. (C) 2008 Elsevier Ltd. All rights reserved.",

keywords = "Cysteine protease, Falcipain-2, Malaria, Peptidomimetic, Plasmodium falciparum",

author = "Edite Verissimo and Neil Berry and Peter Gibbons and Cristiano, \{M. Lurdes S.\} and Rosenthal, \{Philip J.\} and Jiri Gut and Steve Ward and O'Neill, \{Paul M.\}",

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AU - Verissimo, Edite

AU - Berry, Neil

AU - Gibbons, Peter

AU - Cristiano, M. Lurdes S.

AU - Rosenthal, Philip J.

AU - Gut, Jiri

AU - Ward, Steve

AU - O'Neill, Paul M.

PY - 2008/7/15

Y1 - 2008/7/15

N2 - The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. (C) 2008 Elsevier Ltd. All rights reserved.

AB - The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. (C) 2008 Elsevier Ltd. All rights reserved.

KW - Cysteine protease

KW - Falcipain-2

KW - Malaria

KW - Peptidomimetic

KW - Plasmodium falciparum

U2 - 10.1016/j.bmcl.2008.05.068

DO - 10.1016/j.bmcl.2008.05.068

M3 - Article

SN - 0960-894X

VL - 18

SP - 4210

EP - 4214

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 14

ER -

Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors

Abstract

Keywords

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