A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters† †Electronic supplementary information (ESI) available: Experimental procedures, spectral data of new compounds, see DOI: 10.1039/c5ob02630j. Additional data related to this publication is available at the University of Cambridge data repository (https://www.repository.cam.ac.uk/handle/1810/253375). Click here for additional data file.

نویسندگان

  • Petar O. Nikiforov
  • Sachin Surade
  • Michal Blaszczyk
  • Vincent Delorme
  • Priscille Brodin
  • Alain R. Baulard
  • Tom L. Blundell
  • Chris Abell
چکیده

Petar O. Nikiforov,a Sachin Surade,b Michal Blaszczyk,b Vincent Delorme,c Priscille Brodin,c Alain R. Baulard,c Tom L. Blundell,b Chris Abella* a Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, CB2 1EW, UK b Department of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge, CB2 1GA, UK c Inserm U1019 – CNRS UMR 8204, Institut Pasteur de Lille, Université de Lille, 1 rue du Professeur Calmette, 59019, Lille, France

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A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters.

With the ever-increasing instances of resistance to frontline TB drugs there is the need to develop novel strategies to fight the worldwide TB epidemic. Boosting the effect of the existing second-line antibiotic ethionamide by inhibiting the mycobacterial transcriptional repressor protein EthR is an attractive therapeutic strategy. Herein we report the use of a fragment based drug discovery app...

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Laboratory of Molecular Recognition an Zhejiang University, Hangzhou 310027, Zh ac.cn State Key Laboratory of Organometallic C Chemistry, Chinese Academy of Sciences, [email protected] Shanghai Key Laboratory of Magnetic Reson Normal University, Shanghai 200062, P. R. † Electronic supplementary information ( and experimental procedures and theor 979559 and 990983. For ESI and crystallo format s...

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عنوان ژورنال:

دوره 14  شماره 

صفحات  -

تاریخ انتشار 2016