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EXPLORING THE INFLUENCE OF THE SUBSTITUENT AT POSITION 4 IN A SERIES OF 3,4-DIHYDROPYRIMIDIN-2(1H)-ONE A2B ADENOSINE RECEPTOR ANTAGONISTS

Abel Crespo, Abdelaziz El Maatougui, Jhonny Azuaje, Luz Escalante, María Majellaro, María I. Loza, José Brea, María I. Cadavid, Hugo Gutiérrez-de-Terán, Eddy Sotelo
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Abstract


In the context of a program to identify selective adenosine A2B 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 A2B thus highlighting the critical importance of the substituent at position 4 of the 3,4-dihydropyrimidin-2(1H)-one chemotype.


Keywords


3,4-dihydropyrimidin-2(1H)-ones; adenosine antagonists; A2B adenosine receptor; A2B antagonists; structure–activity relationship

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