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Royal Society of Chemistry, Chemical Science, 22(12), p. 7775-7785, 2021

DOI: 10.1039/d1sc00330e

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

Journal article published in 2021 by Ravindra P. Jumde ORCID, Melissa Guardigni, Robin M. Gierse, Alaa Alhayek ORCID, Di Zhu, Zhoor Hamid, Sandra Johannsen ORCID, Walid A. M. Elgaher ORCID, Philipp J. Neusens, Christian Nehls ORCID, Jörg Haupenthal, Norbert Reiling, Anna K. H. Hirsch ORCID
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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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.