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Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A(2B) Adenosine Receptor Antagonists
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2013 (English)In: ACS Medicinal Chemistry Letters, ISSN 1948-5875, E-ISSN 1948-5875, Vol. 4, no 11, 1031-1036 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2013. Vol. 4, no 11, 1031-1036 p.
Keyword [en]
Adenosine antagonists, A(2B) receptor antagonists, 3, 4-dihydropyrimidin-2(1H)-ones, Biginelli reaction
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Medical and Health Sciences
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URN: urn:nbn:se:uu:diva-212869DOI: 10.1021/ml400185vISI: 000327110700003OAI: oai:DiVA.org:uu-212869DiVA: diva2:679991
Available from: 2013-12-17 Created: 2013-12-16 Last updated: 2017-12-06Bibliographically approved

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Gutierrez-de-Teran, Hugo

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