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
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
منابع مشابه
A multistep continuous flow synthesis machine for the preparation of pyrazoles via a metal-free amine-redox process† †Raw spectra can be found at https://www.repository.cam.ac.uk/handle/1810/252343. ‡ ‡Electronic supplementary information (ESI) available. See DOI: 10.1039/c5re00082c Click here for additional data file. Click here for additional data file.
A versatile multistep continuous flow setup is reported for the four-step conversion of anilines into pyrazole products. The synthesis machine incorporates the use of amine-redox chemistry through diazotization and a metal-free vitamin C mediated reduction. The machine can be used for the synthesis of an array of analogues or the scale up of an individual target.
متن کاملA 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