Novel Peptidomimetics Containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors
- Publikationstyp:
- Zeitschriftenaufsatz
- Metadaten:
-
- Autoren
- Roberta Ettari
- Nicola Micale
- Tanja Schirmeister
- Christoph Gelhaus
- Matthias Leippe
- Emanuela Nizi
- Maria Emilia Di Francesco
- Silvana Grasso
- Maria Zappala
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000264835800038&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1021/jm900047j
- Externe Identifier
- Clarivate Analytics Document Solution ID: 428GK
- PubMed Identifier: 19296600
- ISSN
- 0022-2623
- Ausgabe der Veröffentlichung
- 7
- Zeitschrift
- JOURNAL OF MEDICINAL CHEMISTRY
- Paginierung
- 2157 - 2160
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Titel
- Novel Peptidomimetics Containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors
- Sub types
- Article
- Ausgabe der Zeitschrift
- 52
Datenquelle: Web of Science (Lite)
- Andere Metadatenquellen:
-
- Autoren
- Roberta Ettari
- Nicola Micale
- Tanja Schirmeister
- Christoph Gelhaus
- Matthias Leippe
- Emanuela Nizi
- Maria Emilia Di Francesco
- Silvana Grasso
- Maria Zappalà
- DOI
- 10.1021/jm900047j
- eISSN
- 1520-4804
- ISSN
- 0022-2623
- Ausgabe der Veröffentlichung
- 7
- Zeitschrift
- Journal of Medicinal Chemistry
- Sprache
- en
- Online publication date
- 2009
- Paginierung
- 2157 - 2160
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Herausgeber
- American Chemical Society (ACS)
- Herausgeber URL
- http://dx.doi.org/10.1021/jm900047j
- Datum der Datenerfassung
- 2023
- Titel
- Novel Peptidomimetics Containing a Vinyl Ester Moiety as Highly Potent and Selective Falcipain-2 Inhibitors
- Ausgabe der Zeitschrift
- 52
Datenquelle: Crossref
- Abstract
- This paper describes the synthesis and biological evaluation of a new class of peptidomimetic falcipain-2 inhibitors based on a 1,4-benzodiazepine scaffold combined with various alpha,beta-unsaturated electrophilic functions such as vinyl-ketone, -amide, -ester, and -nitrile. The profile of reactivity of this class of derivatives has been evaluated and 4c, containing a vinyl ester warhead, proved to be a highly potent and selective falcipain-2 inhibitor.
- Addresses
- Dipartimento Farmaco-Chimico, University of Messina, Viale Annunziata, Messina, Italy. rettari@pharma.unime.it
- Autoren
- Roberta Ettari
- Nicola Micale
- Tanja Schirmeister
- Christoph Gelhaus
- Matthias Leippe
- Emanuela Nizi
- Maria Emilia Di Francesco
- Silvana Grasso
- Maria Zappalà
- DOI
- 10.1021/jm900047j
- eISSN
- 1520-4804
- Externe Identifier
- PubMed Identifier: 19296600
- Open access
- false
- ISSN
- 0022-2623
- Ausgabe der Veröffentlichung
- 7
- Zeitschrift
- Journal of medicinal chemistry
- Schlüsselwörter
- Cell Line
- Caco-2 Cells
- Animals
- Humans
- Mice
- Plasmodium falciparum
- Esters
- Vinyl Compounds
- Benzodiazepines
- Cathepsins
- Cathepsin B
- Cysteine Endopeptidases
- Peptides
- Recombinant Proteins
- Cysteine Proteinase Inhibitors
- Antimalarials
- Cell Membrane Permeability
- Molecular Mimicry
- Catalytic Domain
- Structure-Activity Relationship
- Cathepsin L
- Sprache
- eng
- Medium
- Paginierung
- 2157 - 2160
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum der Datenerfassung
- 2009
- Titel
- Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
- Sub types
- Research Support, Non-U.S. Gov't
- Journal Article
- Ausgabe der Zeitschrift
- 52
Datenquelle: Europe PubMed Central
- Abstract
- This paper describes the synthesis and biological evaluation of a new class of peptidomimetic falcipain-2 inhibitors based on a 1,4-benzodiazepine scaffold combined with various alpha,beta-unsaturated electrophilic functions such as vinyl-ketone, -amide, -ester, and -nitrile. The profile of reactivity of this class of derivatives has been evaluated and 4c, containing a vinyl ester warhead, proved to be a highly potent and selective falcipain-2 inhibitor.
- Autoren
- Roberta Ettari
- Nicola Micale
- Tanja Schirmeister
- Christoph Gelhaus
- Matthias Leippe
- Emanuela Nizi
- Maria Emilia Di Francesco
- Silvana Grasso
- Maria Zappalà
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/19296600
- DOI
- 10.1021/jm900047j
- eISSN
- 1520-4804
- Ausgabe der Veröffentlichung
- 7
- Zeitschrift
- J Med Chem
- Schlüsselwörter
- Animals
- Antimalarials
- Benzodiazepines
- Caco-2 Cells
- Catalytic Domain
- Cathepsin B
- Cathepsin L
- Cathepsins
- Cell Line
- Cell Membrane Permeability
- Cysteine Endopeptidases
- Cysteine Proteinase Inhibitors
- Esters
- Humans
- Mice
- Molecular Mimicry
- Peptides
- Plasmodium falciparum
- Recombinant Proteins
- Structure-Activity Relationship
- Vinyl Compounds
- Sprache
- eng
- Country
- United States
- Paginierung
- 2157 - 2160
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2009
- Titel
- Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
- Sub types
- Journal Article
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 52
Datenquelle: PubMed
- Beziehungen:
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