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Development of novel inhibitors of the anti-infective target DXS using dynamic combinatorial chemistry (DCC)

Total Cost €


EC-Contrib. €






 NovInDXS project word cloud

Explore the words cloud of the NovInDXS project. It provides you a very rough idea of what is the project "NovInDXS" about.

scaffolds    humans    heterocyclic    2c    plasmodium    unprecedented    cell    fulfil    maximise    falciparum    time    entirely    methicillin    space    assays    economical    urgently    resistant    vivo    pathogens    tuberculosis    explore    heterocycles    selective    aureus    candidates    biochemical    anti    blocks    active    health    idnetifiying    identification    care    methyl    phosphate    hit    chiral    serious    few    benefits    aeruginosa    parts    drug    action    mycobacterium    bacteria    globally    dcc    first    strategy    medically    building    erythritol    discovery    dxs    hitherto    staphylococcus    pioneer    pseudomonas    situation    date    efforts    mode    reported    alarming    none    inhibitors    dynamic    ideal    chances    unexplored    underexplored    chemistry    despite    infective    global    substantial    chemical    bacterial    tested    candidate    combinatorial    compounds    agents    enzyme    absent    emergence    potent    union    socio    hence   

Project "NovInDXS" data sheet

The following table provides information about the project.


Organization address
postcode: 38124

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country Germany [DE]
 Total cost 171˙460 €
 EC max contribution 171˙460 € (100%)
 Programme 1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
 Code Call H2020-MSCA-IF-2017
 Funding Scheme MSCA-IF-EF-ST
 Starting year 2018
 Duration (year-month-day) from 2018-03-01   to  2020-05-26


Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 


 Project objective

The emergence of multi-drug resistant pathogens is a serious global problem. In this alarming situation, novel targets for which inhibitors with an unprecedented mode of action can be developed are urgently required. This proposal aims at the development of selective and potent inhibitors of the important and underexplored anti-infective target DXS, an enzyme from the 2C-methyl-D-erythritol 4-phosphate pathway that is entirely absent in humans but is essential for medically relevant pathogens (e.g., Plasmodium falciparum, Mycobacterium tuberculosis, Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus). Despite substantial efforts dedicated to the discovery of inhibitors for DXS, to date very few active compounds have been reported and none of them fulfil the requirements as an ideal candidate for further development. To address these issues and maximise the chances of success, we will use dynamic combinatorial chemistry (DCC) as a hit identification strategy for the first time for the enzyme-DXS. To explore hitherto unexplored parts of the chemical space, we will pioneer the use of chiral heterocyclic building blocks in DCC for the discovery of potent inhibitors of the enzyme DXS. Use of chiral heterocycles in DCC will allow to rapidly access novel scaffolds. These chiral heterocyclic scaffolds will be evaluated for their biochemical activity on bacterial DXS. The most promising candidates will be tested in in vivo cell-based assays in bacteria. The proposed approach for the design of chiral heterocyclic inhibitors for novel targets such as the enzyme DXS will enhance the knowledge about this underexplored target and will open up access to various potent inhibitors. Hence, this research programme will greatly improve the chances of idnetifiying new anti-infective agents with a novel mode of action, leading to socio-economical benefits for the health care sector in the European Union and also globally.

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The information about "NOVINDXS" are provided by the European Opendata Portal: CORDIS opendata.

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