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Inside Cover: In Vivo Dearomatization of the Potent Antituberculosis Agent BTZ043 via Meisenheimer Complex Formation (Angew. Chem. Int. Ed. 8/2017)
Author(s) -
Kloss Florian,
Krchnak Viktor,
Krchnakova Anna,
Schieferdecker Sebastian,
Dreisbach Julia,
Krone Volker,
Möllmann Ute,
Hoelscher Michael,
Miller Marvin J.
Publication year - 2017
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201700069
Subject(s) - mycobacterium tuberculosis , chemistry , in vivo , nitro , stereochemistry , mycobacterium avium complex , combinatorial chemistry , antibiotics , tuberculosis , microbiology and biotechnology , biochemistry , organic chemistry , biology , medicine , alkyl , pathology
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 on page 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.