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Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies.
Jung, Sascha; Fuchs, Natalie; Johe, Patrick; Wagner, Annika; Diehl, Erika; Yuliani, Tri; Zimmer, Collin; Barthels, Fabian; Zimmermann, Robert A; Klein, Philipp; Waigel, Waldemar; Meyr, Jessica; Opatz, Till; Tenzer, Stefan; Distler, Ute; Räder, Hans-Joachim; Kersten, Christian; Engels, Bernd; Hellmich, Ute A; Klein, Jochen; Schirmeister, Tanja.
Afiliação
  • Jung S; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Fuchs N; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Johe P; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Wagner A; Department of Chemistry, Biochemistry Section, Johannes Gutenberg University, Hanns-Dieter-Hüsch-Weg 17, 55128 Mainz, Germany.
  • Diehl E; Department of Chemistry, Biochemistry Section, Johannes Gutenberg University, Hanns-Dieter-Hüsch-Weg 17, 55128 Mainz, Germany.
  • Yuliani T; Institute for Pharmacology and Clinical Pharmacy, Goethe University, Max-von-Laue-Str. 9, 60439 Frankfurt, Germany.
  • Zimmer C; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Barthels F; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Zimmermann RA; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Klein P; Department of Chemistry, Organic Chemistry Section, Johannes Gutenberg University, Duesbergweg 10-14, 55128 Mainz, Germany.
  • Waigel W; Department of Physical and Theoretical Chemistry, Julius-Maximilians-University, Emil-Fischer-Str. 42, 97074 Würzburg, Germany.
  • Meyr J; Department of Physical and Theoretical Chemistry, Julius-Maximilians-University, Emil-Fischer-Str. 42, 97074 Würzburg, Germany.
  • Opatz T; Department of Chemistry, Organic Chemistry Section, Johannes Gutenberg University, Duesbergweg 10-14, 55128 Mainz, Germany.
  • Tenzer S; Institute for Immunology, University Medical Center, Johannes Gutenberg University, Langenbeckstraße 1, 55131 Mainz, Germany.
  • Distler U; Institute for Immunology, University Medical Center, Johannes Gutenberg University, Langenbeckstraße 1, 55131 Mainz, Germany.
  • Räder HJ; Max Planck Institute for Polymer Research, Ackermannweg 10, 55128 Mainz, Germany.
  • Kersten C; Institute of Pharmaceutical and Biomedical Sciences (IPBS), Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany.
  • Engels B; Department of Physical and Theoretical Chemistry, Julius-Maximilians-University, Emil-Fischer-Str. 42, 97074 Würzburg, Germany.
  • Hellmich UA; Department of Chemistry, Biochemistry Section, Johannes Gutenberg University, Hanns-Dieter-Hüsch-Weg 17, 55128 Mainz, Germany.
  • Klein J; Center for Biomolecular Magnetic Resonance (BMRZ), Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.
  • Schirmeister T; Institute for Pharmacology and Clinical Pharmacy, Goethe University, Max-von-Laue-Str. 9, 60439 Frankfurt, Germany.
J Med Chem ; 64(16): 12322-12358, 2021 08 26.
Article em En | MEDLINE | ID: mdl-34378914
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Sulfonas / Ácidos Sulfônicos / Tripanossomicidas / Compostos de Vinila / Cisteína Endopeptidases / Inibidores de Cisteína Proteinase Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Alemanha
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Sulfonas / Ácidos Sulfônicos / Tripanossomicidas / Compostos de Vinila / Cisteína Endopeptidases / Inibidores de Cisteína Proteinase Limite: Animals / Female / Humans / Male Idioma: En Revista: J Med Chem Assunto da revista: QUIMICA Ano de publicação: 2021 Tipo de documento: Article País de afiliação: Alemanha