Design and synthesis of conformationally constraint Dyrk1A inhibitors by creating an intramolecular H-bond involving a benzothiazole core
Author:
Affiliation:
1. Pharmaceutical and Medicinal Chemistry
2. Saarland University
3. D-66123 Saarbrücken
4. Germany
5. Department of Pharmaceutical Chemistry
6. Faculty of Pharmacy and Biotechnology
7. German University in Cairo
8. Cairo 11835
9. Egypt
Abstract
We present the development of conformationally pre-organised Dyrk1A inhibitors based on the hydroxybenzothiazole urea scaffold.
Funder
Deutsche Forschungsgemeinschaft
Publisher
Royal Society of Chemistry (RSC)
Subject
Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2018/MD/C8MD00142A
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1. Sequence Characteristics, Subcellular Localization, and Substrate Specificity of DYRK-related Kinases, a Novel Family of Dual Specificity Protein Kinases
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4. The DYRK1A gene, encoded in chromosome 21 Down syndrome critical region, bridges between β-amyloid production and tau phosphorylation in Alzheimer disease
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