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American Chemical Society, ACS Medicinal Chemistry Letters, 11(4), p. 1031-1036, 2013

DOI: 10.1021/ml400185v

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

Journal article published in 2013 by Abel Crespo, Hugo Gutiérrez de-Terán, Abdelaziz El Maatougui, Abdelaziz El Maatougui, Pierfrancesco Biagini, Jhonny Azuaje, Alberto Coelho ORCID, José Brea, María Isabel Loza ORCID, María Isabel Cadavid, Xerardo García-Mera, Hugo Gutiérrez-De-Terán, Eddy Sotelo
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This paper is available in a repository.

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Abstract

We describe the discovery and optimization of 3,4-dihydropyrimidin-2(1H)-ones as a novel family of (nonzanthine) A(2B) 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 hA(2B) AdoR affinity and remarkable selectivity profiles.