2. Academic Validation
  3. Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists

Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists

  • ACS Med Chem Lett. 2013 Oct 3;4(11):1031-6. doi: 10.1021/ml400185v.
Abel Crespo 1,  Abdelaziz El Maatougui 1,  Pierfrancesco Biagini 2,  Jhonny Azuaje 1,  Alberto Coelho 1,  José Brea 2,  María Isabel Loza 2,  María Isabel Cadavid 2,  Xerardo García-Mera 2,  Hugo Gutiérrez-de-Terán 3,  Eddy Sotelo 4
Affiliations

Affiliations

  • 1 Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain ; Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain.
  • 2 Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain.
  • 3 Department of Cell and Molecular Biology, Uppsala University, Biomedical Center , Uppsala SE-75124, Sweden.
  • 4 Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain ; Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain ; Center for Research in Biological Chemistry and Molecular Materials (CIQUS), Institute of Industrial Pharmacy, Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela , Santiago de Compostela 15782, Spain.
PMID: 24900602 DOI: 10.1021/ml400185v
Abstract

We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)-ones as a novel family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity profile. The Biginelli-based hit optimization process enabled a thoughtful exploration of the structure-activity and structure-selectivity relationships for this chemotype, enabling the identification of ligands that combine structural simplicity with excellent hA2B AdoR affinity and remarkable selectivity profiles.

Keywords

3,4-dihydropyrimidin-2(1H)-ones; A2B receptor antagonists; Adenosine antagonists; Biginelli reaction.

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