Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A2B adenosine receptor antagonists

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Abstract

The synthesis and SAR of a series of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent A2B adenosine receptor antagonists is described. Several compounds showed good selectivity versus other adenosine receptors. The potent and selective analogue 9 was shown to have good oral bioavailability in the rat.

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The potent and selective A2B adenosine receptor antagonist 9 was shown to have good oral bioavailability in the rat.

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Acknowledgements

We thank Maria Isabel Loza and Maria Isabel Cadavid from the Universidad de Santiago de Compostela for performing the radioligand binding assays mentioned in this work.

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