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  Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones

Madikizela, B., Eckhardt, T., Goddard, R., Richter, A., Lins, A., Lehmann, C., et al. (2021). Synthesis, structural characterization and antimycobacterial evaluation of several halogenated non-nitro benzothiazinones. Medicinal Chemistry Research, 30(8), 1523-1533. doi:10.1007/s00044-021-02735-4.

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Madikizela, Balungile1, 2, Autor
Eckhardt, Tamira1, Autor
Goddard, Richard3, Autor           
Richter, Adrian1, 4, Autor
Lins, Anika1, Autor
Lehmann, Christoph1, Autor
Imming, Peter1, Autor
Seidel, Rüdiger W.1, Autor
Affiliations:
1Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, Wolfgang-Langenbeck-Str. 4, Halle (Saale) 06120, Germany, ou_persistent22              
2Phytomedicine Programme, Department of Paraclinical Sciences, University of Pretoria, Private Bag X04, Onderstepoort 0110, South Africa, ou_persistent22              
3Service Department Lehmann (EMR), Max-Planck-Institut für Kohlenforschung, Max Planck Society, ou_1445625              
4Department of Medicine and Department of Microbiology and Immunology, University of British Columbia, Vancouver, BC V6T 1Z3, Canada, ou_persistent22              

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Schlagwörter: Benzothiazinones; Tuberculosis; Antimycobacterial evaluation; in vitro activity; Synthesis; Crystal structure
 Zusammenfassung: 8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new
class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-D-ribose-2′-epimerase (DprE1),
an enzyme crucial for cell wall synthesis in the pathogen Mycobacterium tuberculosis. Synthesis, structural
characterization and in vitro testing against Mycobacterium aurum DSM 43999 and M. tuberculosis H37Rv of
halogenated 2-(4-ethoxycarbonylpiperazin-1-yl)-1,3-benzothiazin-4-ones lacking a nitro group are reported. X-ray
crystallography reveals that the structure of the BTZ scaffold can significantly deviate from planarity. In contrast to recent
reports, the results of the present study indicate that further investigation of halogenated non-nitro BTZs for antitubercular
activity is less than a promising approach.

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Sprache(n): eng - English
 Datum: 2021-03-312021-06-102021-08-01
 Publikationsstatus: Erschienen
 Seiten: 11
 Ort, Verlag, Ausgabe: -
 Inhaltsverzeichnis: -
 Art der Begutachtung: Expertenbegutachtung
 Identifikatoren: DOI: 10.1007/s00044-021-02735-4
 Art des Abschluß: -

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Titel: Medicinal Chemistry Research
  Kurztitel : Med. Chem. Res.
Genre der Quelle: Zeitschrift
 Urheber:
Affiliations:
Ort, Verlag, Ausgabe: New York : Springer
Seiten: - Band / Heft: 30 (8) Artikelnummer: - Start- / Endseite: 1523 - 1533 Identifikator: ISSN: 1054-2523
CoNE: https://pure.mpg.de/cone/journals/resource/1054-2523