Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase-Reference-Cited by-同舟云学术

Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase

Published:2021 Issue:22 Volume:12 Page:7775-7785
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Jumde Ravindra P.¹²³⁴^ORCID,Guardigni Melissa¹²³⁴⁵,Gierse Robin M.¹²³⁴⁶,Alhayek Alaa¹²³⁴⁶^ORCID,Zhu Di¹²³⁴⁶,Hamid Zhoor¹²³⁴⁶^ORCID,Johannsen Sandra¹²³⁴⁶^ORCID,Elgaher Walid A. M.¹²³⁴^ORCID,Neusens Philipp J.¹²³⁴⁶,Nehls Christian⁷⁸⁹¹⁰⁴^ORCID,Haupenthal Jörg¹²³⁴,Reiling Norbert¹¹⁸⁹¹⁰⁴,Hirsch Anna K. H.¹²³⁴⁶^ORCID

Affiliation:

1. Department of Drug Design and Optimization

2. Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) – Helmholtz Centre for Infection Research (HZI)

3. 66123 Saarbrücken

4. Germany

5. D3-PharmaChemistry, Istituto Italiano di Tecnologia

6. Department of Pharmacy

7. RG Biophysics

8. Research Center Borstel

9. Leibniz Lung Center

10. Borstel

11. RG Microbial Interface Biology

Abstract

Target-directed dynamic combinatorial chemistry was used for hit-identification and subsequent hit-optimization for the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase resulting in novel inhibitors with low micromolar affinities.

Funder

Nederlandse Organisatie voor Wetenschappelijk Onderzoek

Horizon 2020 Framework Programme

H2020 European Research Council

Helmholtz Association

Schlumberger Foundation

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/SC/D1SC00330E