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Issue 6, 2018
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Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core

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Abstract

We present the development of conformationally pre-organised Dyrk1A inhibitors based on the hydroxybenzothiazole urea scaffold. The modifications introduced to the discovered hit (AHS-211) proved the crucial role of the urea linker to preserve the bioactive conformation and led to the development of compound b5 as a promising selective Dyrk1A inhibitor.

Graphical abstract: Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core

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Publication details

The article was received on 14 Mar 2018, accepted on 27 May 2018 and first published on 28 May 2018


Article type: Research Article
DOI: 10.1039/C8MD00142A
Citation: Med. Chem. Commun., 2018,9, 1045-1053
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    Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core

    M. Salah, M. Abdel-Halim and M. Engel, Med. Chem. Commun., 2018, 9, 1045
    DOI: 10.1039/C8MD00142A

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