Inside Cover: In Vivo Dearomatization of the Potent Antituberculosis Agent BTZ043 via Meisenheimer Complex Formation (Angew. Chem. Int. Ed. 8/2017). Issue 8 (26th January 2017)

• Record Type: Journal Article
• Authors: Kloss, Florian; Krchnak, Viktor; Krchnakova, Anna; Schieferdecker, Sebastian; Dreisbach, Julia; Krone, Volker; Möllmann, Ute; Hoelscher, Michael; Miller, Marvin J.
• Is Part Of: Angewandte Chemie international edition. Volume 56:Issue 8(2017)
• Page Start: 1932
• Page End: 1932
• Publication Date: 2017-01-26
• Subjects: benzothiazinones -- DprE1 inhibitors -- metabolite identification -- prodrugs -- transient metabolites; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201700069
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract : Nitrobenzothiazinones are highly potent antibiotics against Mycobacterium tuberculosis . While their killing mechanism involves the reduction of the nitro to a reactive nitroso group, F. Kloss and co‐workers describe in their Communication onpage 2187 ff. a previously overlooked in vivo bioreduction pathway. The metabolites are transient hydride Meisenheimer complexes that are readily reoxidized under atmospheric conditions and completely unprecedented among drug metabolites.