BIP! Finder - Design and Microwave Synthesis of New (5Z) 5-Arylidene-2-thioxo-1,3-thiazolinidin-4-one and (5Z) 2-Amino-5-arylidene-1,3-thiazol-4(5H)-one as New Inhibitors of Protein Kinase DYRK1A

2021 • Design and Microwave Synthesis of New (5Z) 5-Arylidene-2-thioxo-1,3-thiazolinidin-4-one and (5Z) 2-Amino-5-arylidene-1,3-thiazol-4(5H)-one as New Inhibitors of Protein Kinase DYRK1A

Authors: Khadidja Bourahla, Solène Guihéneuf, Emmanuelle Limanton, Ludovic Paquin, Rémy Le Guével, Thierry Charlier, Mustapha Rahmouni, Emilie Durieu, Olivier Lozach, François Carreaux, Laurent Meijer, Jean Pierre Bazureau

Venue: Pharmaceuticals

Type: Publication

Abstract: Here, we report on the synthesis of libraries of new 5-arylidene-2-thioxo-1,3-thiazolidin-4-ones 3 (twenty-two compounds) and new 2-amino-5-arylidene-1,3-thiazol-4(5H)-ones 5 (twenty-four compounds) with stereo controlled Z-geometry under microwave irradiation. The 46 designed final compounds were tested in order to determine their activity against four representative protein kinases (DYR1A, CK1, CDK5/p25, and GSK3α/β). Among these 1,3-thiazolidin-4-ones, the molecules (5Z) 5-(4-hydroxybenzylidene)-2-thioxo-1,3-thiazolidin-4-one 3e (IC(50) 0.... (read more)

Topics: Stereochemistry Combinatorial chemistry

DOI: 10.3390/ph14111086

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External links: Crossref OpenAIRE

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