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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 (engelsk)Inngår i: ACS Medicinal Chemistry Letters, ISSN 1948-5875, E-ISSN 1948-5875, Vol. 4, nr 11, s. 1031-1036Artikkel i tidsskrift (Fagfellevurdert) 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.

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2013. Vol. 4, nr 11, s. 1031-1036
Emneord [en]
Adenosine antagonists, A(2B) receptor antagonists, 3, 4-dihydropyrimidin-2(1H)-ones, Biginelli reaction
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Identifikatorer
URN: urn:nbn:se:uu:diva-212869DOI: 10.1021/ml400185vISI: 000327110700003OAI: oai:DiVA.org:uu-212869DiVA, id: diva2:679991
Tilgjengelig fra: 2013-12-17 Laget: 2013-12-16 Sist oppdatert: 2017-12-06bibliografisk kontrollert

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