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4. Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors

Author

UCL - SSS/LDRI - Louvain Drug Research Institute, Prevost, Julien R.C., Kozlova, Arina, Es Saadi, Bouazza, Yildiz, Esra, Modaffari, Sara, Lambert, Didier M., Pochet, Lionel, Wouters, Johan, Dolušić, Eduard, Frédérick, Raphaël, UCL - SSS/LDRI - Louvain Drug Research Institute, Prevost, Julien R.C., Kozlova, Arina, Es Saadi, Bouazza, Yildiz, Esra, Modaffari, Sara, Lambert, Didier M., Pochet, Lionel, Wouters, Johan, Dolušić, Eduard, and Frédérick, Raphaël

Abstract

Highly functionalized 5-bromo-2-amino-1,3-thiazoles bearing various substituents could be easily prepared by a rapid and efficient one-pot method, using simple starting materials and mild conditions while avoiding the use of metal catalysts or inconvenient reagents such as elemental halogens. These useful products can serve as starting materials for other reactions or as pharmacologically interesting compounds. In our work we have shown that the resulting 5-bromothiazole compounds could lead to monoacylglycerol lipase (MAGL) inhibition in the lM range.

Published
2018

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