Synthesis and biological evaluation of novel imidazole-containing macrocycles

Nshimyumukiza, Prosper;Van Den Berge, Emilie;Delest, Bruno;Mijatovic, Tatjana;Robiette, Raphaël;et.al.
(2010) Tetrahedron — Vol. 66, n° 25, p. 4515-4520 (2010)

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Authors
  • Nshimyumukiza, ProsperUCLouvain
    Author
  • Van Den Berge, EmilieUCLouvain
    Author
  • Delest, BrunoUCLouvain
    Author
  • Mijatovic, TatjanaUniv Libre Bruxelles
    Author
  • Marchand-Brynaert, JacquelineUCLouvain
    Author
  • Robiette, Raphaëlorcid-logoUCLouvain
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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 A(3) adenosine (h) receptor, dopamine D-1 (h) receptor, chloride channel (GABA-gated), and choline transporter (h) CHT1. (C) 2010 Elsevier Ltd. All rights reserved.
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Nshimyumukiza, P., Van Den Berge, E., Delest, B., Mijatovic, T., Kiss, R., Marchand-Brynaert, J., & Robiette, R. (2010). Synthesis and biological evaluation of novel imidazole-containing macrocycles. Tetrahedron, 66(25), 4515-4520. https://doi.org/10.1016/j.tet.2010.04.070 (Original work published 2010)