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Exploring the influence of the substituent at position 4 in a series of 3,4-dihydropyrimidin-2(1H)-one A(2B) adenosine receptor antagonists
Univ Santiago de Compostela, Ctr Singular Invest Quim Biol & Mat Mol CIQUS, Santiago De Compostela 1578, Spain.;Univ Santiago de Compostela, Fac Farm, Dept Quim Organ, Santiago De Compostela 1578, Spain..
Univ Santiago de Compostela, Ctr Singular Invest Quim Biol & Mat Mol CIQUS, Santiago De Compostela 1578, Spain.;Univ Santiago de Compostela, Fac Farm, Dept Quim Organ, Santiago De Compostela 1578, Spain..
Univ Santiago de Compostela, Ctr Singular Invest Quim Biol & Mat Mol CIQUS, Santiago De Compostela 1578, Spain.;Univ Santiago de Compostela, Fac Farm, Dept Quim Organ, Santiago De Compostela 1578, Spain..
Univ Santiago de Compostela, Ctr Singular Invest Quim Biol & Mat Mol CIQUS, Santiago De Compostela 1578, Spain.;Univ Santiago de Compostela, Fac Farm, Dept Quim Organ, Santiago De Compostela 1578, Spain..
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2017 (English)In: Chemistry of Heterocyclic Compounds, ISSN 0009-3122, E-ISSN 1573-8353, Vol. 53, no 3, 316-321 p.Article in journal (Refereed) Published
Abstract [en]

In the context of a program to identify selective adenosine A(2B) receptor antagonists, we have obtained a focused library of 4-substituted 3,4-dihydropyrimidin-2(1H)-ones and its affinity for the four human adenosine receptor subtypes was determined. The synthesis was accomplished by using an experimentally simple and efficient Biginelli approach. The biological evaluation of the library revealed that all the documented derivatives exhibit low or negligible affinity for the A(2B) receptor, thus highlighting the critical importance of the substituent at position 4 of the 3,4-dihydropyrimidin-2(1H)-one chemotype.

Place, publisher, year, edition, pages
Springer, 2017. Vol. 53, no 3, 316-321 p.
Keyword [en]
3, 4-dihydropyrimidin-2(1H)-ones, adenosine antagonists, A(2B) adenosine receptor, A(2B) antagonists, structure-activity relationship
National Category
Organic Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-323667DOI: 10.1007/s10593-017-2054-4ISI: 000400545300009OAI: oai:DiVA.org:uu-323667DiVA: diva2:1112656
Available from: 2017-06-20 Created: 2017-06-20 Last updated: 2017-06-20Bibliographically approved

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Gutiérrez-de-Terán, Hugo
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