Abstract
We herein report the discovery of a novel class of antagonists of the human adenosine A2B receptor. This low molecular weight scaffold has been optimized to offer derivatives with potential utility for the alleviation of conditions associated with this receptor subtype, such as nociception, diabetes, asthma and COPD. Furthermore, preliminary pharmacokinetic analysis has revealed compounds with profiles suitable for either inhaled or systemic routes of administration.
MeSH terms
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Adenosine A2 Receptor Antagonists*
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Administration, Inhalation
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Animals
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Asthma / drug therapy
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Drug Design
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Humans
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Pulmonary Disease, Chronic Obstructive / drug therapy
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacokinetics
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Rats
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Receptor, Adenosine A2A / metabolism
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Receptor, Adenosine A2B / metabolism
Substances
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Adenosine A2 Receptor Antagonists
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Pyrimidines
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Receptor, Adenosine A2A
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Receptor, Adenosine A2B
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thienopyrimidine