Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors
| Autor: | Esra Yildiz, Eduard Dolusic, Johan Wouters, Bouazza Es Saadi, Sara Modaffari, Julien R. C. Prevost, Lionel Pochet, Didier M. Lambert, Raphaël Frédérick, Arina Kozlova |
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| Přispěvatelé: | UCL - SSS/LDRI - Louvain Drug Research Institute |
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
Halogenation
010405 organic chemistry Chemistry Organic Chemistry Electrophilic aromatic substitution Monoacylglycerol lipase 010402 general chemistry 01 natural sciences Combinatorial chemistry Endocannabinoid system Biochemistry 0104 chemical sciences Thiazoles Reagent Oxidation Hydrolase Drug Discovery Metal catalyst |
| Zdroj: | Tetrahedron Letters, Vol. 59, no.49, p. 4315-4319 (2018) |
| Popis: | 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 μM range. |
| Databáze: | OpenAIRE |
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