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Synthesis and biological evaluation of novel imidazole-containing macrocycles |
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| Authors: | Prosper Nshimyumukiza Emilie Van Den Berge Tatjana Mijatovic Jacqueline Marchand-Brynaert |
| Affiliation: | a Institute of Condensed Matter and Nanosciences, Université catholique de Louvain, Place Louis Pasteur 1, B-1348 Louvain-la-Neuve, Belgium b Unibioscreen SA, 40 avenue Joseph Wibran, B-1070 Brussels, Belgium c Institute of Pharmacy, Université Libre de Bruxelles, Campus Plaine CP205-1, Blvd du Triomphe, B-1050 Brussels, Belgium |
| Abstract: | A new family of compounds made of a 5-aryl-1H-imidazole motif included in a macrocycle has been designed and synthesized. The synthesis of the imidazole core makes use of our previously developed method for the regioselective preparation of 1,2,5-trisubstituted imidazoles while the construction of the macrocycle is based on a three steps sequence: SNAr, Suzuki coupling, and RCM reaction. Biological evaluation of synthesized imidazole-containing macrocycles revealed that they display actual binding activity toward A3 adenosine (h) receptor, dopamine D1 (h) receptor, chloride channel (GABA-gated), and choline transporter (h) CHT1. |
| Keywords: | Central nervous system Conformational flexibility Imidazole Inflammation Macrocycles |
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