Ontology highlight
ABSTRACT:
SUBMITTER: Makarov V
PROVIDER: S-EPMC4505264 | biostudies-literature | 2015 Aug
REPOSITORIES: biostudies-literature
Makarov Vadim V Neres João J Hartkoorn Ruben C RC Ryabova Olga B OB Kazakova Elena E Šarkan Michal M Huszár Stanislav S Piton Jérémie J Kolly Gaëlle S GS Vocat Anthony A Conroy Trent M TM Mikušová Katarína K Cole Stewart T ST
Antimicrobial agents and chemotherapy 20150518 8
8-Nitro-benzothiazinones (BTZs), such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. Structure-activity relationship (SAR) studies revealed the 8-nitro group of the BTZ scaffold to be crucial for the mechanism of action, which involves formation of a semimercaptal bond with Cys387 in the active site of DprE1. To date, substitution of the 8-nitro group has led to extensive l ...[more]