Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines,a promising privileged structure |
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Authors: | Rajaa Boulahjar Angela Rincon Arias Raphaël Bolteau Nicolas Renault Mathilde Coevoet Amélie Barczyk Romain Duroux Saïd Yous Patricia Melnyk Laurence Agouridas |
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Affiliation: | 1. Univ. Lille, Inserm, CHU Lille, UMR-S 1172 JPArc Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer, F-59000 Lille, France;2. Univ. Lille, Inserm, CHU Lille, U995 LIRIC Lille Inflammation Research International Center, F-59000 Lille, France |
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Abstract: | Imidazo[1,2a]pyridines have gained much interest in the field of medicinal chemistry research. In the aim of accessing new privileged structure, we decided to design and synthesize 8-aminated-imidazo[1,2a]pyridines substituted on positions 2 and 6. This scaffold, rarely found in the literature, was obtained via palladium-catalyzed coupling reactions (Suzuki reaction or N-hydroxysuccinimidyl activated ester method) and tested on adenosine receptor A2A. We demonstrated how incorporation of an exocyclic amine enhanced affinity towards this receptor while maintaining low cytotoxicity. |
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Keywords: | Privileged structure Amino-imidazopyridine Palladium-catalyzed coupling reaction |
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