Ontology highlight
ABSTRACT:
SUBMITTER: Xia Y
PROVIDER: S-EPMC6238539 | biostudies-literature | 2018 Jun
REPOSITORIES: biostudies-literature
Xia Yi Y Zhou Yasheen Y Carter David S DS McNeil Matthew B MB Choi Wai W Halladay Jason J Berry Pamela W PW Mao Weimin W Hernandez Vincent V O'Malley Theresa T Korkegian Aaron A Sunde Bjorn B Flint Lindsay L Woolhiser Lisa K LK Scherman Michael S MS Gruppo Veronica V Hastings Courtney C Robertson Gregory T GT Ioerger Thomas R TR Sacchettini Jim J Tonge Peter J PJ Lenaerts Anne J AJ Parish Tanya T Alley Mrk M
Life science alliance 20180601 3
New antitubercular agents are needed to combat the spread of multidrug- and extensively drug-resistant strains of <i>Mycobacterium tuberculosis</i>. The frontline antitubercular drug isoniazid (INH) targets the mycobacterial enoyl-ACP reductase, InhA. Resistance to INH is predominantly through mutations affecting the prodrug-activating enzyme KatG. Here, we report the identification of the diazaborines as a new class of direct InhA inhibitors. The lead compound, AN12855, exhibited in vitro bacte ...[more]