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

doi:10.1021/acs.jmedchem.1c01002

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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, S., Fuchs, N., Johe, P., Wagner, A., Diehl, E., Yuliani, T., et al. (2021). Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure–Activity Relationship, Inhibition Mechanism, Metabolism, and In Vivo Studies. Journal of Medicinal Chemistry, 64(16), 12322-12358. doi:10.1021/acs.jmedchem.1c01002.

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Item Permalink: https://hdl.handle.net/21.11116/0000-0009-2DA2-E Version Permalink: https://hdl.handle.net/21.11116/0000-0009-2DA3-D

Genre: Journal Article

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Creators:
Jung, Sascha^{1, 2}, Author
Fuchs, Natalie¹, Author
Johe, Patrick¹, Author
Wagner, Annika^{3, 4, 5}, Author
Diehl, Erika³, Author
Yuliani, Tri^{6, 7}, Author
Zimmer, Collin¹, Author
Barthels, Fabian¹, Author
Zimmermann, Robert A.¹, Author
Klein, Philipp⁸, Author
Waigel, Waldemar⁹, Author
Meyr, Jessica⁹, Author
Opatz, Till⁸, Author
Tenzer, Stefan¹⁰, Author
Distler, Ute¹⁰, Author
Räder, Hans Joachim¹¹, Author
Kersten, Christian¹, Author
Engels, Bernd⁹, Author
Hellmich, Ute A.^{3, 4, 5, 12}, Author
Klein, Jochen⁶, Author
Schirmeister, Tanja¹, Author more..

Affiliations:
1Johannes Gutenberg Univ Mainz, Inst Pharmaceut & Biomed Sci IPBS, Mainz, Germany, ou_persistent22
2TU Dortmund, Fac Chem & Chem Biol, Dortmund, Germany, ou_persistent22
3Johannes Gutenberg Univ Mainz, Dept Chem, Biochem Sect, Mainz, Germany, ou_persistent22
4Friedrich Schiller Univ, Inst Organ Chem & Macromol Chem IOMC, Germany, ou_persistent22
5Friedrich Schiller Univ Jena, Cluster Excellence Balance Microverse, Jena, Germany, ou_persistent22
6Goethe Univ, Inst Pharmacol & Clin Pharm, Frankfurt, Germany, ou_persistent22
7Indonesian Inst Sci LIPI, Res Ctr Chem, Gd 452 Kawasan PUSPIPTEK, Tangerang Selatan, Indonesia, ou_persistent22
8Johannes Gutenberg Univ Mainz, Dept Chem, Organ Chem Sect, Mainz, Germany, ou_persistent22
9Julius Maximilians Univ, Dept Phys & Theoret Chem, Würzburg, Germany, ou_persistent22
10Johannes Gutenberg Univ Mainz, Univ Med Ctr, Inst Immunol, Mainz, Germany, ou_persistent22
11Dept. Weil: Synthesis of Macromolecules, MPI for Polymer Research, Max Planck Society, ou_2301691
12Goethe Univ, Ctr Biomol Magnet Resonance BMRZ, Frankfurt, Germany, ou_persistent22

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Language(s): eng - English

Dates: Published Online: 2021-08-11Date issued: 2021-08-26

Publication Status: Issued

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Identifiers: DOI: 10.1021/acs.jmedchem.1c01002

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Title: Journal of Medicinal Chemistry

Source Genre: Journal

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Publ. Info: Washington DC : ACS Publications

Pages: - Volume / Issue: 64 (16) Sequence Number: - Start / End Page: 12322 - 12358 Identifier: ISSN: 0022-2623
CoNE: https://pure.mpg.de/cone/journals/resource/110992357271168