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N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: The First Example of Adenosine-Related Structures With Potent Agonist Activity at the Human A(2B) Adenosine Receptor

N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: The First Example of Adenosine-Related Structures With Potent Agonist Activity at the Human A(2B) Adenosine Receptor

Pier Giovanni Baraldi, Delia Preti, Mojgan Aghazadeh Tabrizi, Francesca Fruttarolo, Giulia Saponaro, Stefania Baraldi, Romeo Romagnoli, Allan R Moorman, Stefania Gessi, Katia Varani, Pier Andrea Borea

Bioorg Med Chem. 2007 Apr 1;15(7):2514-27.

PMID: 17306548

Abstract:

A new series of N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines (24-43) has been synthesised and tested in binding assays at hA(1), hA(2A) and hA(3) adenosine receptors, and in a functional assay at the hA(2B) subtype. The examined compounds displayed high potency in activating A(2B) receptors with good selectivity versus A(2A) subtypes. The introduction of an unsubstituted 4-[(phenylcarbamoyl)-methoxy]-phenyl chain at the N(6) position of 5'-N-ethylcarboxamido-adenosine led us to the recognition of compound 24 as a full agonist displaying the highest efficacy of the series (EC(50) hA(2B)=7.3 nM). These compounds represent the first report about adenosine-related structures capable of activating hA(2B) subtype in the low nanomolar range.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP35920399	5′-(N-Ethylcarboxamido)adenosine		35920-39-9	Price

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