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Evaluation of bisbenzamidines as inhibitors for matriptase-2.
Beckmann, Anna-Madeleine; Gilberg, Erik; Gattner, Susanne; Huang, Tien L; Vanden Eynde, Jean Jacques; Mayence, Annie; Bajorath, Jürgen; Stirnberg, Marit; Gütschow, Michael.
Afiliação
  • Beckmann AM; Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
  • Gilberg E; Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany; Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology and Medicinal Chemistry, University of Bonn, Dahlmannstr. 2, 53113 Bonn, Germany.
  • Gattner S; Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
  • Huang TL; Department of Basic Pharmaceutical Science, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA.
  • Vanden Eynde JJ; Department of Basic Pharmaceutical Science, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA.
  • Mayence A; Department of Basic Pharmaceutical Science, College of Pharmacy, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA.
  • Bajorath J; Department of Life Science Informatics, B-IT, LIMES Program Unit Chemical Biology and Medicinal Chemistry, University of Bonn, Dahlmannstr. 2, 53113 Bonn, Germany.
  • Stirnberg M; Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
  • Gütschow M; Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, 53121 Bonn, Germany.
Bioorg Med Chem Lett ; 26(15): 3741-5, 2016 08 01.
Article em En | MEDLINE | ID: mdl-27287367
The serine protease matriptase-2 has attracted much attention as a potential target for the treatment of iron overload diseases. In this study, a series of 27 symmetric, achiral bisbenzamidines was evaluated for inhibitory activity against human matriptase-2, against the closely related enzyme human matriptase, as well as against human thrombin, bovine factor Xa and human trypsin. The conformationally restricted piperazine derivative 19 and the oxamide-derived bisbenzamidine 1 were identified as the most potent inhibitors of this series for matriptase-2 and matriptase, respectively.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidinas / Inibidores de Serina Proteinase / Proteínas de Membrana Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
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XML
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidinas / Inibidores de Serina Proteinase / Proteínas de Membrana Idioma: En Ano de publicação: 2016 Tipo de documento: Article