Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors
- Publication type:
- Journal article
- Metadata:
-
- Autoren
- Nicola Micale
- Roberta Ettari
- Tanja Schirmeister
- Astrid Evers
- Christoph Gelhaus
- Matthias Leippe
- Maria Zappala
- Silvana Grasso
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000269399700003&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1016/j.bmc.2009.08.013
- eISSN
- 1464-3391
- Externe Identifier
- Clarivate Analytics Document Solution ID: 489DK
- PubMed Identifier: 19709887
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 18
- Zeitschrift
- BIOORGANIC & MEDICINAL CHEMISTRY
- Schlüsselwörter
- Cysteine proteases
- Falcipain-2 inhibitors
- 2H-Isoquinolin-3-ones
- Paginierung
- 6505 - 6511
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Titel
- Novel 2<i>H</i>-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors
- Sub types
- Article
- Ausgabe der Zeitschrift
- 17
Data source: Web of Science (Lite)
- Other metadata sources:
-
- Autoren
- Nicola Micale
- Roberta Ettari
- Tanja Schirmeister
- Astrid Evers
- Christoph Gelhaus
- Matthias Leippe
- Maria Zappalà
- Silvana Grasso
- DOI
- 10.1016/j.bmc.2009.08.013
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 18
- Zeitschrift
- Bioorganic & Medicinal Chemistry
- Sprache
- en
- Paginierung
- 6505 - 6511
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Herausgeber
- Elsevier BV
- Herausgeber URL
- http://dx.doi.org/10.1016/j.bmc.2009.08.013
- Datum der Datenerfassung
- 2019
- Titel
- Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors
- Ausgabe der Zeitschrift
- 17
Data source: Crossref
- Abstract
- A series of 1-aryl-6,7-disubstituted-2H-isoquinolin-3-ones (2-10) was synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2, as well as against cultured P. falciparum strain FCBR parasites. All compounds displayed inhibitory activity against recombinant falcipain-2 and against in vitro cultured intraerythrocytic P. falciparum, with the exception of 9. The new compounds exhibited no selectivity against human cysteine proteases such as cathepsins B and L. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense.
- Addresses
- Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata 98168, Messina, Italy. nmicale@pharma.unime.it
- Autoren
- Nicola Micale
- Roberta Ettari
- Tanja Schirmeister
- Astrid Evers
- Christoph Gelhaus
- Matthias Leippe
- Maria Zappalà
- Silvana Grasso
- DOI
- 10.1016/j.bmc.2009.08.013
- eISSN
- 1464-3391
- Externe Identifier
- PubMed Identifier: 19709887
- Open access
- false
- ISSN
- 0968-0896
- Ausgabe der Veröffentlichung
- 18
- Zeitschrift
- Bioorganic & medicinal chemistry
- Schlüsselwörter
- Animals
- Humans
- Plasmodium falciparum
- Trypanosoma brucei rhodesiense
- Malaria, Falciparum
- Isoquinolines
- Cysteine Endopeptidases
- Cysteine Proteinase Inhibitors
- Antiprotozoal Agents
- Parasitic Sensitivity Tests
- Structure-Activity Relationship
- Sprache
- eng
- Medium
- Print-Electronic
- Online publication date
- 2009
- Paginierung
- 6505 - 6511
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum der Datenerfassung
- 2009
- Titel
- Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.
- Sub types
- Research Support, Non-U.S. Gov't
- Journal Article
- Ausgabe der Zeitschrift
- 17
Data source: Europe PubMed Central
- Abstract
- A series of 1-aryl-6,7-disubstituted-2H-isoquinolin-3-ones (2-10) was synthesized and evaluated for their inhibition against Plasmodium falciparum cysteine protease falcipain-2, as well as against cultured P. falciparum strain FCBR parasites. All compounds displayed inhibitory activity against recombinant falcipain-2 and against in vitro cultured intraerythrocytic P. falciparum, with the exception of 9. The new compounds exhibited no selectivity against human cysteine proteases such as cathepsins B and L. The inhibitory activity of the synthesized compounds was also evaluated against another protozoal cysteine protease, namely rhodesain of Trypanosoma brucei rhodesiense.
- Date of acceptance
- 2009
- Autoren
- Nicola Micale
- Roberta Ettari
- Tanja Schirmeister
- Astrid Evers
- Christoph Gelhaus
- Matthias Leippe
- Maria Zappalà
- Silvana Grasso
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/19709887
- DOI
- 10.1016/j.bmc.2009.08.013
- eISSN
- 1464-3391
- Ausgabe der Veröffentlichung
- 18
- Zeitschrift
- Bioorg Med Chem
- Schlüsselwörter
- Animals
- Antiprotozoal Agents
- Cysteine Endopeptidases
- Cysteine Proteinase Inhibitors
- Humans
- Isoquinolines
- Malaria, Falciparum
- Parasitic Sensitivity Tests
- Plasmodium falciparum
- Structure-Activity Relationship
- Trypanosoma brucei rhodesiense
- Sprache
- eng
- Country
- England
- Paginierung
- 6505 - 6511
- PII
- S0968-0896(09)00764-0
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2009
- Titel
- Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.
- Sub types
- Journal Article
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 17
Data source: PubMed
- Beziehungen:
- Property of