The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma

Adenosine has been suggested to play a role in asthma, possibly via activation of A(2B) adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A(2B) AdoR antagonist that resulted in the discovery of CVT-5440, a high affinit...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-02, Vol.15 (3), p.609-612
Hauptverfasser:	Zablocki, Jeff, Kalla, Rao, Perry, Thao, Palle, Venkata, Varkhedkar, Vaibhav, Xiao, Dengming, Piscopio, Anthony, Maa, Tenning, Gimbel, Art, Hao, Jia, Chu, Nancy, Leung, Kwan, Zeng, Dewan
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine A2 Receptor Antagonists Asthma - drug therapy Drug Stability Humans Liver - cytology Liver - metabolism Structure-Activity Relationship Xanthines - chemical synthesis Xanthines - pharmacology
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Zusammenfassung:	Adenosine has been suggested to play a role in asthma, possibly via activation of A(2B) adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A(2B) AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A(2B) AdoR antagonist with good selectivity (A(2B) AdoR K(i)=50 nM, selectivity A(1)>200: A(2A)>200: A(3)>167).
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2004.11.044